- A new aza-BODIPY based NIR region colorimetric and fluorescent chemodosimeter for fluoride
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The synthesis and characterization of a novel NIR region fluoride sensor, that makes use of the aza-boron-dipyrromethene (aza-BODIPY) fluorophore, is described. An arylmagnesium bromide was formed by reacting 4-bromophenol with a tert-butyldimethylsilyl p
- Zou, Bin,Liu, Hui,Mack, John,Wang, Sisi,Tian, Jiangwei,Lu, Hua,Li, Zhifang,Shen, Zhen
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Read Online
- Synthesis and characteristics of novel TPA-containing electrochromic poly(ether sulfone)s with dimethylamino substituents
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Newly designed dimethylamine-substituted triphenylamine (TPA) derivatives, N,N'-(1,4-phenylene)bis(N-(4-((tert-butyldimethylsilyl)oxy)phenyl)-N'',N''-dimethylbenzene-1,4-diamine) (NTPPA-2Si) and N,N'-((1,1′-biphenyl)-4,4′-diyl)bis(N-(4-((tert-butyldimethy
- Huang, Chiao-Ling,Kung, Yu-Ruei,Liou, Guey-Sheng,Shao, Yu-Jen
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Read Online
- Use of Silylated Formiates as Hydrosilane Equivalents
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The present invention relates to a method for preparing organic compounds of formula (I) by reaction between a silylated formiate of formula (II) and an organic compound in the presence of a catalyst and optionally of an additive. The invention also relates to use of the method for preparing organic compounds of formula (I) for the preparation of reagents for fine chemistry and for heavy chemistry, as well as in the production of vitamins, pharmaceutical products, adhesives, acrylic fibres, synthetic leathers, and pesticides.
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Paragraph 0514
(2021/09/26)
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- Structure-Activity Relationship and Mode-Of-Action Studies Highlight 1-(4-Biphenylylmethyl)-1H-imidazole-Derived Small Molecules as Potent CYP121 Inhibitors
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CYP121 of Mycobacterium tuberculosis (Mtb) is an essential target for the development of novel potent drugs against tuberculosis (TB). Besides known antifungal azoles, further compounds of the azole class were recently identified as CYP121 inhibitors with
- Walter, Isabell,Adam, Sebastian,Gentilini, Maria Virginia,Kany, Andreas M.,Brengel, Christian,Thomann, Andreas,Sparwasser, Tim,K?hnke, Jesko,Hartmann, Rolf W.
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p. 2786 - 2801
(2021/06/27)
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- Acylative desymmetrization of cyclic meso-1,3-diols by chiral DMAP derivatives
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An efficient enantioselective acylative desymmetrization of cyclic meso-1,3-diols was developed by using a chiral DMAP derivative 1e having a 1,1¤-binaphthyl unit. The reactions required only 0.5mol% of the catalyst and showed good to excellent enantioselectivity. With this transformation, 5a, a key building block for the synthesis of natural products, was easily obtained in almost enantiomerically pure form after a single recrystallization. Control experiments revealed that tert-alcohol units on the catalyst were responsible for both the catalytic activity and enantioselectivity.
- Mandai, Hiroki,Hironaka, Tsubasa,Mitsudo, Koichi,Suga, Seiji
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supporting information
p. 471 - 474
(2021/03/15)
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- Polymerizable compounds. Liquid crystal composition and liquid crystal display device
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A polymerizable compound having a formula of formula (I): Ring A, ring B, Z1 , Z2 , R, P, n And m are as described in the specification and the application patent range, respectively. The liquid crystal composition containing the pol
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Paragraph 0079-0080
(2021/09/08)
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- Fenton chemistry for Achmatowicz rearrangement
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Achmatowicz rearrangement (AchR) is a very important transformation for the synthesis of various heterocyclic building blocks and natural products. Here, the discovery of Fenton chemistry for AchR using a bifunctional catalyst (FeBr2 or CeBrsu
- Zhao, Guodong,Liang, Lixin,Wang, Eryu,Tong, Rongbiao
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p. 3740 - 3748
(2021/04/07)
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- Green bromination method
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The invention discloses a green bromination method, and belongs to the field of green organic chemistry. Under the conditions of room temperature, opening and neutrality, reaction raw materials are aromatic hydrocarbon, olefin, alkyne, tryptamine, tryptophane and derivatives thereof with different functional groups, a bromine source is MBrx (M is Fe , Fe , Ce and the like, and x is 2-3), and the unique oxidant is H2O2. Brominated alkanes, alkenes, aromatic hydrocarbons, pyrrolo-indolines and furo-indolines and derivatives thereof can be produced. The bromination reaction is carried out by using easily available and cheap reagents (such as FeBr2, CeB3 and H2O2) in the market and the solvent, and the method has the characteristics of mild reaction conditions, wide substrate application range, simple steps, easiness in operation and no need of separation, is a green, environment-friendly and safe bromination reaction method, and has a good application prospect.
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Paragraph 0035-0037
(2021/06/13)
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- Carbosulfenylation of Alkenes with Organozinc Reagents and Dimethyl(methylthio)sulfonium Trifluoromethanesulfonate
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The electrophilic alkylthiolation of alkenes, initiated by dimethyl(methylthio)sulfonium salts and the subsequent addition of various heteronucleophilies has been well-established. Regarding the use of carbon nucleophiles, however, only carefully designed sp-type carbon sources have been successfully applied. We herein present our findings on the methylthiolation of alkenes with dimethyl(methylthio)sulfonium trifluoromethanesulfonate, followed by carbon-carbon bond formation in the presence of organozinc reagents, thus achieving a catalyst-free protocol toward to the carbosulfenylation of alkenes.
- Tang, Meizhong,Han, Shuxiong,Huang, Shenglan,Huang, Shenlin,Xie, Lan-Gui
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supporting information
p. 9729 - 9734
(2020/12/21)
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- Shuttling Catalyst: Facilitating C?C Bond Formation via Cross-Couplings with a Thermoresponsive Polymeric Ligand
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A poly(ethylene glycol) (PEG) linked ortho-MeO-phenyldicyclohexylphosphine (MeO-WePhos) ligand has been synthesized to promote Pd-catalyzed carbon-carbon bond formation by cross-couplings including Sonogashira, Heck, Hiyama and Stille reactions, providing corresponding (hetero)aryl substituted alkynes, alkenes and bi(hetero)aryls in good to excellent isolated yields with low Pd loadings. Facilitated by the lower critical solution temperature behaviour of the polymeric monophosphine ligand, the metal-complex could rapidly shuttle between organic and water phases as regulated by temperature, enabling highly efficient catalyst recycling via a simple phase separation. The chemical structure of ligand was determined by matrix-assisted laser desorption/ionization-time of flight mass spectrometry, nuclear magnetic resonance spectrometry and size-exclusion chromatography measurements. Notably, as demonstrated by the inductively coupled plasma-atomic emission spectrometry measurement, 98% Pd was kept in the water phase after 6 cycles of catalyst recycling experiments. Given the profound impact of transition-metal-catalyzed covalent bond formation and the increasing demand of sustainable chemistry, this work provides an alternative method to conduct cross-couplings with a polymeric shuttling catalyst.
- Wang, Erfei,Zhang, Jiawei,Zhong, Zhuoran,Chen, Kaixuan,Chen, Mao
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p. 419 - 423
(2020/01/08)
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- Catalyst shuttling enabled by a thermoresponsive polymeric ligand: Facilitating efficient cross-couplings with continuously recyclable ppm levels of palladium
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A polymeric monophosphine ligand WePhos has been synthesized and complexed with palladium(ii) acetate [Pd(OAc)2] to generate a thermoresponsive pre-catalyst that can shuttle between water and organic phases, with the change being regulated by temperature. The structure of the polymeric ligand was confirmed with matrix-assisted laser desorption/ionization-time-of-flight (MALDI-TOF) mass spectrometry and size-exclusion chromatography (SEC) analysis, as well as nuclear magnetic resonance (NMR) measurements. This polymeric metal complex enables highly efficient Pd-catalyzed cross-couplings and tandem reactions using 50 to 500 ppm palladium, and this can facilitate reactions that are tolerant to a broad spectrum of (hetero)aryl substrates and functional groups, as demonstrated with 73 examples with up to 99% isolated yields. Notably, 97% Pd remained in the aqueous phase after 10 runs of catalyst recycling experiments, as determined via inductively coupled plasma-atomic emission spectrometry (ICP-AES) measurements, indicating highly efficient catalyst transfer. Furthermore, a continuous catalyst recycling approach has been successfully developed based on flow chemistry in combination with the catalyst shuttling behavior, allowing Suzuki-Miyaura couplings to be conducted at gram-scales with as little as 10 ppm Pd loading. Given the significance of transition-metal catalyzed cross-coupling and increasing interest in sustainable chemistry, this work is an important step towards the development of a responsive catalyst, in addition to having high activity, by tuning the structures of the ligands using polymer science.
- Wang, Erfei,Chen, Mao
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p. 8331 - 8337
(2019/09/30)
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- Ni-Catalyzed Reductive Cyanation of Aryl Halides and Phenol Derivatives via Transnitrilation
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Herein, we report a Ni-catalyzed reductive coupling for the synthesis of benzonitriles from aryl (pseudo)halides and an electrophilic cyanating reagent, 2-methyl-2-phenyl malononitrile (MPMN). MPMN is a bench-stable, carbon-bound electrophilic CN reagent that does not release cyanide under the reaction conditions. A variety of medicinally relevant benzonitriles can be made in good yields. Addition of NaBr to the reaction mixture allows for the use of more challenging aryl electrophiles such as aryl chlorides, tosylates, and triflates. Mechanistic investigations suggest that NaBr plays a role in facilitating oxidative addition with these substrates.
- Mills, L. Reginald,Graham, Joshua M.,Patel, Purvish,Rousseaux, Sophie A. L.
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supporting information
p. 19257 - 19262
(2019/12/02)
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- Preparation method of 4-(4-hydroxyphenyl) cyclohexanone
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The invention relates to the technical field of chemical synthesis, in particular to a preparation method of 4-(4-hydroxyphenyl) cyclohexanone. According to the preparation method, p-bromophenol is used as a raw material, a Grignard reagent is prepared through hydroxyl protection and Grignard reaction, then the prepared Grignard reagent is utilized to couple with 1,4-cyclohexanedione monoethyleneglycol ketal, then the product is dehydrated to obtain alkene, and double protecting groups are removed after hydrogenation to prepare a target product, namely, 4-(4-hydroxyphenyl) cyclohexanone. Thepreparation method of 4-(4-hydroxyphenyl) cyclohexanone, provided by the invention, has the advantages of reasonable process design, high yield and low production cost; the prepared 4-(4-hydroxyphenyl) cyclohexanone is a white solid, the HPLC content is more than 99.5%, the total yield of the product can reach 75-80%, and the raw materials are easy to obtain; and the method has simple operation and high safety, and realizes industrial production of 4-(4-hydroxyphenyl) cyclohexanone.
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Paragraph 0088-0091
(2019/08/01)
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- Diaryl hydroxylamines as pan or dual inhibitors of indoleamine 2,3-dioxygenase-1, indoleamine 2,3-dioxygenase-2 and tryptophan dioxygenase
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Tryptophan (Trp) catabolizing enzymes play an important and complex role in the development of cancer. Significant evidence implicates them in a range of inflammatory and immunosuppressive activities. Whereas inhibitors of indoleamine 2,3-dioxygenase-1 (IDO1) have been reported and analyzed in the clinic, fewer inhibitors have been described for tryptophan dioxygenase (TDO) and indoleamine 2,3-dioxygenase-2 (IDO2) which also have been implicated more recently in cancer, inflammation and immune control. Consequently the development of dual or pan inhibitors of these Trp catabolizing enzymes may represent a therapeutically important area of research. This is the first report to describe the development of dual and pan inhibitors of IDO1, TDO and IDO2.
- Winters, Maria,DuHadaway, James B.,Pham, Khoa N.,Lewis-Ballester, Ariel,Badir, Shorouk,Wai, Jenny,Sheikh, Eesha,Yeh, Syun-Ru,Prendergast, George C.,Muller, Alexander J.,Malachowski, William P.
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supporting information
p. 455 - 464
(2018/11/25)
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- THERAPEUTIC COMPOUNDS AND USES THEREOF
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The present invention relates to compounds useful in the modulation of ion channel activity in cells. The invention also relates to use of these compounds in the treatment of pain, and pharmaceutical compositions containing these compounds and methods for their preparation.
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Page/Page column 48; 58
(2019/07/17)
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- SILICON-CONTAINING COMPOUND, LIQUID-CRYSTAL COMPOSITION AND LIQUID-CRYSTAL DISPLAY USING THE SAME
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A silicon-containing compound, liquid-crystal composition and a liquid-crystal display using the silicon-containing compound are provided. The silicon-containing compound has a structure represented by Formula (I): wherein K, R1, A1,
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Paragraph 0151; 0152
(2019/11/19)
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- A solvent- and temperature-dependent intramolecular equilibrium of diamagnetic and paramagnetic states in Co complexes bearing triaryl amines
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Complexes [Co(L)2](ClO4)2 (L = o-substituted 2-(pyridine-2-yl)-1,10-phenanthrolines 1a-c) containing three redox active centres (a Co2+ ion and two triaryl amine (Tara) units) have been synthesised. The order of
- Schnaubelt, Linda,Petzold, Holm,Dmitrieva, Evgenia,Rosenkranz, Marco,Lang, Heinrich
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supporting information
p. 13180 - 13189
(2018/10/02)
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- Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen – A new hybrid design paradigm
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Hybrid antiestrogen/histone deacetylase (HDAC) inhibitors were designed by appending zinc binding groups to the 4-hydroxystilbene core of 4-hydroxytamoxifen. The resulting hybrids were fully bifunctional, and displayed high nanomolar to low micromolar IC
- Palermo, Anthony F.,Diennet, Marine,El Ezzy, Mohamed,Williams, Benjamin M.,Cotnoir-White, David,Mader, Sylvie,Gleason, James L.
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supporting information
p. 4428 - 4440
(2018/08/06)
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- Total Synthesis, Stereochemical Assignment, and Divergent Enantioselective Enzymatic Recognition of Larreatricin
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A concise and efficient total synthesis of the lignan natural product larreatricin as well as an unambiguous assignment of configuration of its enantiomers are reported, resolving a long-held controversy. Enzyme kinetic studies revealed that different polyphenol oxidases show high and remarkably divergent enantioselective recognition of this secondary metabolite.
- Martin, Harry J.,Kampatsikas, Ioannis,Oost, Rik,Pretzler, Matthias,Al-Sayed, Emir,Roller, Alexander,Giester, Gerald,Rompel, Annette,Maulide, Nuno
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supporting information
p. 15756 - 15760
(2018/10/09)
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- Organocatalytic Nitroaldol Reaction Associated with Deuterium-Labeling
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A deuterium-labeling reaction of nitroalkanes in deuterium oxide and the subsequent nitroaldol reaction have been accomplished under basic and organocatalytic conditions to provide the deuterium-labeled β-nitroalcohols in high yields and high deuterium contents. β-Deuterated β-nitroalcohols could be smoothly obtained from the reaction of nitroalkanes and various electrophiles using the easily-removal basic resin WA30. Furthermore, the asymmetric nitroaldol reaction using nitromethane and α-keto esters as electrophiles in the presence of a quinine-derived organocatalyst in deuterium oxide could provide the desired β-deuterated nitroalcohol derivatives with high enantioselectivities. (Figure presented.).
- Yamada, Tsuyoshi,Kuwata, Marina,Takakura, Ryoya,Monguchi, Yasunari,Sajiki, Hironao,Sawama, Yoshinari
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supporting information
p. 637 - 641
(2017/12/13)
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- NOVEL PROCESS FOR PREPARATION OF EMPAGLIFLOZIN OR ITS CO-CRYSTALS, SOLVATES AND THEIR POLYMORPHS THEREOF
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The present invention relates to process for the preparation of Empagliflozin or its co- crystals, solvates and/or polymorphs thereof. The present invention also relates to novel intermediates used therein, and process for the preparation thereof. The pre
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Page/Page column 38
(2019/01/06)
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- Silylation of O-H bonds by catalytic dehydrogenative and decarboxylative coupling of alcohols with silyl formates
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The silylation of O-H bonds is a useful methodology in organic synthesis and materials science. While this transformation is commonly achieved by reacting alcohols with reactive chlorosilanes or hydrosilanes, we show herein for the first time that silylformates HCO2SiR3 are efficient silylating agents for alcohols, in the presence of a ruthenium molecular catalyst.
- Chauvier, Clément,Godou, Timothé,Cantat, Thibault
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supporting information
p. 11697 - 11700
(2017/11/03)
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- A general strategy to add diversity to ruthenium arene complexes with bioactive organic compounds: Via a coordinated (4-hydroxyphenyl)diphenylphosphine ligand
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Esterification of (4-hydroxyphenyl)diphenylphosphine, coordinated to the [Ru(η6-p-cymene)Cl2] fragment, allows a series of bioactive carboxylic acids to be introduced directly into the organometallic molecule. Evaluation of the compounds on human ovarian cancer cells reveals synergistic enhancements in their antiproliferative activity relative to their bioactive organic and organometallic precursors.
- Biancalana, Lorenzo,Batchelor, Lucinda K.,De Palo, Alice,Zacchini, Stefano,Pampaloni, Guido,Dyson, Paul J.,Marchetti, Fabio
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supporting information
p. 12001 - 12004
(2017/09/25)
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- Containing diphenylacetylene cyclopentadienyl iron salt such two-photon absorbing material and its preparation method
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The invention relates to three cyclopentadienyl iron salt two-photon absorption materials having a diphenylacetylene group and a preparation method thereof; a diphenylacetylene structure and a cationic cyclopentadienyl iron receptor are jointly composed of a D-(pi)-A type two-photon absorption functional group, and thus the three synthesized novel cyclopentadienyl iron salts have a strong two-photon absorption ability at 532 nm, and has great application value in the two-photon photoetching field when used as the two-photon absorption type cationic photo-initiator.
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Paragraph 0042-0044; 0054; 0055
(2017/08/25)
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- HISTONE DEMETHYLASE INHIBITORS
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The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrido[3,4-d]pyrimidin-4-one derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
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Paragraph 00250; 00293
(2016/04/09)
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- An efficient and chemoselective deprotection of aryl tert-butyldimethylsilyl (TBDMS) ethers by NaCN
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Phenolic tert-butyldimethylsilyl (TBDMS) ethers can be deprotected to yield phenols in excellent yield using sodium cyanide (NaCN) as catalyst in ethanol. The deprotectation of various phenolic TBDMS ethers were found to be very convenient, fast, high yielding and chemoselective.
- Qiao, Xue-Jun,Hou, Xiao,Fang, Wu-Hong,Bao, Xue-Fei,Chen, Guo-Liang
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p. 899 - 904
(2016/05/19)
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- Light-Triggered RNA Annealing by an RNA Chaperone
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Non-coding antisense RNAs regulate bacterial genes in response to nutrition or environmental stress, and can be engineered for artificial gene control. The RNA chaperone Hfq accelerates antisense pairing between non-coding RNAs and their mRNA targets, by a mechanism still unknown. We used a photocaged guanosine derivative in an RNA oligonucleotide to temporally control Hfq catalyzed annealing. Using a fluorescent molecular beacon as a reporter, we observed RNA duplex formation within 15 s following irradiation (3 s) of photocaged RNA complexed with Hfq. The results showed that the Hfq chaperone directly stabilizes the initiation of RNA base pairs, and suggests a strategy for light-activated control of gene expression by non-coding RNAs.
- Panja, Subrata,Paul, Rakesh,Greenberg, Marc M.,Woodson, Sarah A.
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supporting information
p. 7281 - 7284
(2015/06/30)
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- SUBSTITUTED FUSED HETEROCYCLES AS GPR119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS
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The present invention relates to substituted fused heterocyclic compounds. The substituted fused heterocyclic compounds are GPR1 19 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of substituted fused heterocyclic compounds as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
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Page/Page column 53; 54
(2015/11/17)
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- ISOINDOLINONE COMPOUNDS AS GPR119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS
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The present invention relates to isoindolinone compounds. The isoindolinone compounds are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the u
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Page/Page column 69
(2015/11/02)
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- Strategies for large-scale synthesis of coelenterazine for in vivo applications
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A new application of two Negishi-type coupling reactions for the synthesis of coelenterazine is reported. The synthesis of coelenterazine in high purity on a gram scale will enable numerous approaches to bioluminescence imaging and possibly photodynamic therapy of deep-seated tumors. Coelenterazine is the substrate for several luciferases, among them Gaussia luciferase (gLuc). This synthesis starts with pyrazin-2-amine and uses inexpensive starting materials and catalysts. Georg Thieme Verlag Stuttgart New York.
- Shrestha, Tej B.,Troyer, Deryl L.,Bossmann, Stefan H.
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p. 646 - 652
(2014/03/21)
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- S1P AND/OR ATX MODULATING AGENTS
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Compounds of formula (I), and pharmaceutically acceptable salts thereof, can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).
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Paragraph 00254
(2014/06/11)
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- Ti/Ni-mediated inter- and intramolecular conjugate addition of aryl and alkenyl halides and triflates
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In this work, we show that the unique combination of a nickel catalyst and Cp2TiCl allows the direct conjugate addition of aryl and alkenyl iodides, bromides, and to a lesser extent, chlorides and triflates to α,β-unsaturated carbonyls at room temperature, without requiring the previous formation of an organometallic nucleophile. The reaction proceeds inter- and intramolecularly with good functional group compatibility, which is key for the development of free protecting group methodologies. Carbo- and heterocycles of five- and six-membered rings are obtained in good yields. Moreover, some insights about the mechanism involved have been obtained from cyclic voltammetry, UV-vis, and HRTEM measurements.
- Marquez, Irene R.,Miguel, Delia,Millan, Alba,Marcos, M. Luisa,De Cienfuegos, Luis Alvarez,Campana, Araceli G.,Cuerva, Juan M.
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supporting information
p. 1529 - 1541
(2014/03/21)
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- COELENTERAZINE ANALOGUES AND COELENTERAMIDE ANALOGUES
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Coelenterazine analogs with different luminescence properties from conventional ones and coelenteramide analogs with different fluorescence properties from conventional ones have been desired. The invention provides coelenterazine analogs modified at the
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Paragraph 0247; 0248
(2014/10/29)
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- Recycling Pd colloidal catalysts using polymeric phosphine ligands and polyethylene as a solvent
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Polyisobutylene (PIB)-bound azo dyes were prepared from aryl amine terminated polyisobutylene oligomers and used to form palladacycle precatalysts that can be used for catalytic carbon-carbon cross coupling reactions. The catalysts so formed were recyclable using thermomorphic heptane-DMF solutions that are monophasic at 80 °C and biphasic at room temperature. Under these conditions, the Pd catalyst can be recycled but some Pd leaches into the product solution. Using a low melting polyethylene oligomer as a solvent in place of the volatile heptane solvent reduces this leaching by roughly an order of magnitude. Further modification that involves using a second polyisobutylene (PIB)-bound phosphine ligand both increases the activity of the colloidal Pd catalyst and decreases the total Pd leaching by almost two orders of magnitude with 99.88% of the Pd being recovered. In this case, the Pd content in the solution of the product was ca. 0.3 ppm. These two modifications together lead to a much more sustainable strategy for the use of Pd colloidal catalysts in catalytic cross coupling chemistry.
- Priyadarshani, Nilusha,Suriboot, Jakkrit,Bergbreiter, David E.
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supporting information
p. 1361 - 1367
(2013/06/27)
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- Synthesis of macrocyclic ketones exploiting palladium-catalyzed activation of carboxylic acids as an enabling step
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The novel synthesis of macrocyclic arylketones via palladium-catalyzed cross-coupling of arylboronic acids and carboxylic acids, activated by the treatment with di(N-succinimidyl) carbonate, is disclosed. This allows the high yielding synthesis of various
- Kapdi, Anant R.,Fairlamb, Ian J. S.
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p. 961 - 964
(2013/06/27)
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- Increased hydrophobicity and estrogenic activity of simple phenols with silicon and germanium-containing substituents
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Here, we report the systematic synthesis and characterization of simple phenols bearing a trialkyl(aryl)silyl or trialkyl(aryl)germyl functional group as a hydrophobic substituent. These silicon and germanium analogues exhibited higher hydrophobicity than
- Fujii, Shinya,Miyajima, Yu,Masuno, Hiroyuki,Kagechika, Hiroyuki
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p. 160 - 166
(2013/02/23)
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- Enhanced catalytic activity in suzuki-miyaura couplings by shell crosslinked pd nanoparticles from alkene-terminated phosphine dendron-stabilized Pd nanoparticles
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New alkene-terminated phosphine dendron-protected palladium nanoparticles (NPs) have been synthesized, and the olefin metathesis polymerization of their Pd NPs led to shell crosslinked Pd NPs without aggregation of the Pd NPs. The introduction of crosslinking at the surface of the protective ligand enhanced the catalytic activity of the Pd NPs for SuzukiMiyaura couplings.
- Shiomi, Toshiaki,Nakahodo, Tsukasa,Fujihara, Hisashi
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supporting information
p. 1700 - 1702
(2013/02/23)
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- COELENTERAZINE ANALOGUES AND COELENTERAMIDE ANALOGUES
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Coelenterazine analogues with different luminescence properties from conventional ones and coelenteramide analogues with different fluorescence properties from conventional ones have been desired. The invention provides coelenterazine analogues modified at the 8-position of coelenterazine and coelenteramide analogues modified at the 2- or 3-position of coelenteramide.
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- SYNTHESIS OF MORPHINE AND RELATED DERIVATIVES
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The present invention relates to methods for the synthesis of galanthamine, morphine, intermediates, salts and derivatives thereof, wherein the starting compound is biphenyl.
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Page/Page column 67; 71-72
(2010/12/17)
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- Variable-temperature NMR studies of soluble polymer-supported phosphine-silver complexes
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(Chemical Equation Presented) The use of polymers as supports for organometallic catalysts has received wide attention. However, catalyst reactivity is sometimes altered as a consequence of catalyst immobilization by a polymeric ligand and such altered reactivity can complicate such supported catalysts' use. The results in this study show that heptane phase selectively soluble polyisobutylene (PIB)-bound phosphine ligands have essentially identical kinetic behavior when compared to electronically similar isobutyldiphenylphosphine analogues in phosphine coordination and exchange in silver(I) halide complexes. These studies used variable-temperature 31P NMR spectroscopy to probe the silver-phosphine exchange processes for both AgI and AgCl complexes of these polymeric and low molecular weight phosphine ligands. The results show that the dynamic behavior of the PIB- and isobutyldiphenylphosphine-AgX complexes is nearly identical based on line-shape analysis of these 31P NMR spectra as a function of temperature. Similar studies of more polar poly(ethylene glycol)triarylphosphine-bound AgX complexes and electronically analogous low molecular weight AgX complexes have similar behavior in variable-temperature 31P NMR spectroscopy.
- Bergbreiter, David E.,Yang, Yun-Chin
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scheme or table
p. 873 - 878
(2010/04/30)
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- FLUORENE DERIVATIVE, LIQUID CRYSTAL COMPOSITION COMPRISING THE SAME, AND OPTICAL FILM USING THE SAME LIQUID CRYSTAL COMPOSITION
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Disclosed are a novel fluorene derivative, a liquid crystal composition comprising the same, and an optical film using the same liquid crystal composition. More particularly, there are provided a liquid crystal material for a viewing angle compensation fi
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Page/Page column 7-8
(2010/04/23)
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- NOVEL LIQUID CRYSTAL COMPOUND, LIQUID CRYSTAL COMPOSITION COMPRISING THE SAME, AND OPTICAL FILM USING THE SAME LIQUID CRYSTAL COMPOSITION
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Disclosed is a novel liquid crystal compound, a liquid crystal composition comprising the same, and an optical film using the same liquid crystal composition. More particularly, there is provided a liquid crystal material of a viewing angle compensation f
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Page/Page column 7; 8
(2010/04/23)
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- Organic synthesis using a hypervalent iodine reagent: Unexpected and novel domino reaction leading to spiro cyclohexadienone lactones
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The reaction of 1-(p-hydroxyaryl)cyclobutanols and phenyl iodide(iii) diacetate in hexafluoroisopropanol and water produced spiro cyclohexadienone lactones via a domino reaction.
- Fujioka, Hiromichi,Komatsu, Hideyuki,Nakamura, Taeko,Miyoshi, Akihito,Hata, Kayoko,Ganesh, Jnashuara,Murai, Kenichi,Kita, Yasuyuki
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supporting information; scheme or table
p. 4133 - 4135
(2010/09/03)
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- HSP90 INHIBITORS CONTAINING A ZINC BINDING MOIETY
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The present invention relates to HSP90 inhibitors containing a zinc binding moiety and their use in the treatment of cell proliferative diseases such as cancer. The said derivatives may further act as HDAC inhibitors.
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Page/Page column 29; 34-35
(2009/04/24)
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- Concise syntheses of (-)-galanthamine and (±)-codeine via intramolecular alkylation of a phenol derivative
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(Figure Presented). A new solution-processable fabrication protocol using a soluble tetrabenzoporphyrin (BP) precursor and bis(dimethylphenylsilylmethyl) [60]fullerene (SIMEF) created three-layered p-i-n photovoltaic devices, in which the i-layer possesses a well-defined bulk heterojunction structure in which columnar BP crystals grow vertically from the bottom p-layer. The device showed a power conversion efficiency of 5.2% (VOC = 0.75 V; JSC = 10.5 mA/cm2; FF = 0.65).
- Magnus, Philip,Sane, Neeraj,Fauber, Benjamin P.,Lynch, Vince
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supporting information; experimental part
p. 16045 - 16047
(2010/02/16)
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- Novel CYP17 inhibitors: Synthesis, biological evaluation, structure-activity relationships and modelling of methoxy- and hydroxy-substituted methyleneimidazolyl biphenyls
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Recently, the steroidal CYP17 inhibitor Abiraterone entered phase II clinical trial for the treatment of androgen-dependent prostate cancer. As 17α-hydroxylase-17,20-lyase (CYP17) catalyzes the last step in androgen biosynthesis, inhibition of this target should affect not only testicular but also adrenal androgen formation. Therefore CYP17 inhibitors should be advantageous over existing therapies, for example with GnRH analogues. However, steroidal drugs are known for side effects which are due to affinities for steroid receptors. Therefore we decided to synthesize non-steroidal compounds mimicking the natural CYP17 substrates pregnenolone and progesterone. The synthesis and biological evaluation of a series of 15 novel and highly active non-steroidal CYP17 inhibitors are reported. The compounds were prepared via Suzuki-cross-coupling, Grignard reaction and CDI-assisted SNt-reaction with imidazole and their inhibitory activity was examined with recombinant human CYP17 expressed in Escherichia coli. Promising compounds were further tested for their selectivity against the hepatic enzyme CYP3A4 and the glucocorticoid-forming enzyme CYP11B1. All compounds turned out to be potent CYP17 inhibitors. The most active compounds 7 and 8 were much more active than Ketoconazole showing activity comparable to Abiraterone (IC50 values of 90 and 52 nM vs. 72 nM). Most compounds also showed higher selectivities than Ketoconazole, but turned out to be less selective than Abiraterone. Docking studies using our CYP17 protein model were performed with selected compounds to study the interactions between the inhibitors and the amino acid residues of the active site.
- Hille, Ulrike E.,Hu, Qingzhong,Vock, Carsten,Negri, Matthias,Bartels, Marc,Mueller-Vieira, Ursula,Lauterbach, Thomas,Hartmann, Rolf W.
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experimental part
p. 2765 - 2775
(2009/10/09)
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- SILOLE-BASED MONOMERS AND POLYMERS FOR ORGANIC LIGHT-EMITTING DIODE DEVICES
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This invention relates generally to organic electroluminescent norbornene-silole monomers, poly (norbornene) homopolymers, and poly (norbornene) copolymers containing functionalized aryl and alkyl silole side chains having good host characteristics and so
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Page/Page column 17
(2009/07/25)
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- Nanotube composites consisting of metal nanoparticles and polythiophene from electropolymerization of terthiophene-functionalized metal (Au, Pd) nanoparticles
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We have developed a new method for the fabrication of metal nanoparticle/polythiophene nanotube composites, i.e., the template-based electrochemical polymerization of terthiophene-linked oligoethyleneoxy-thiol (1) and -phosphine (2)-stabilized gold and pa
- Umeda, Ryuhei,Awaji, Hiroshi,Nakahodo, Tsukasa,Fujihara, Hisashi
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p. 3240 - 3241
(2008/09/20)
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- Synthesis, biological evaluation, and molecular modeling studies of methylene imidazole substituted biaryls as inhibitors of human 17α-hydroxylase-17,20-lyase (CYP17)-Part II: Core rigidification and influence of substituents at the methylene bridge
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Thirty-five novel substituted imidazolyl methylene biphenyls have been synthesized as CYP17 inhibitors for the potential treatment of prostate cancer. Their activities have been tested with recombinant human CYP17 expressed in Escherichia coli. Promising compounds were tested for selectivity against CYP11B1, CYP11B2, and hepatic CYP enzymes 3A4, 1A2, 2B6 and 2D6. The core rigidified compounds (30-35) were the most active ones, being much more potent than Ketoconazole and reaching the activity of Abiraterone. However, they were not very selective. Another rather potent and more selective inhibitor (compound 23, IC50 = 345 nM) was further examined in rats regarding plasma testosterone levels and pharmacokinetic properties. Compared to the reference Abiraterone, 23 was more active in vivo, showed a longer plasma half-life (10 h) and a higher bioavailability. Using our CYP17 homology protein model, docking studies with selected compounds were performed to study possible interactions between inhibitors and amino acid residues of the active site.
- Hu, Qingzhong,Negri, Matthias,Jahn-Hoffmann, Kerstin,Zhuang, Yan,Olgen, Sureyya,Bartels, Marc,Mueller-Vieira, Ursula,Lauterbach, Thomas,Hartmann, Rolf W.
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p. 7715 - 7727
(2008/12/23)
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- NOVEL LIQUID CRYSTAL COMPOUND, LIQUID CRYSTAL COMPOSITION COMPRISING THE SAME, AND OPTICAL FILM USING THE SAME LIQUID CRYSTAL COMPOSITION
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Disclosed is a novel liquid crystal compound, a liquid crystal composition comprising the same, and an optical film using the same liquid crystal composition. More particularly, there is provided a liquid crystal material of a viewing angle compensation f
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Paragraph 99-101
(2008/12/07)
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