- Enantioselective syntheses of (S)- and (R)-8,9 dihydroxydihydromagnolol
-
8,9-Dihydroxydihydromagnolol 5 was synthesized in four steps in which the synthesis of magnolol 4 was improved and the absolute configuration of 5 was confirmed as (R).
- Gu, Wenxin,She, Xuegong,Pan, Xinfu,Yang, Teng-Kuei
-
-
Read Online
- A Copper-Mediated Conjugate Addition Approach to Analogues of Aconitine-Type Diterpenoid Alkaloids
-
A copper-mediated conjugate addition of electron-rich aryl groups into a complex vinyl nitrile using arylmagnesium bromides is reported. The conjugate addition adducts were advanced toward the synthesis of designed aconitine-type analogues. The variation
- Doering, Nicolle A.,Kou, Kevin G. M.,Norseeda, Krissada,Lee, Jack C.,Marth, Christopher J.,Gallego, Gary M.,Sarpong, Richmond
-
-
Read Online
- Chemistry-oriented synthesis (ChOS) and target deconvolution on neuroprotective effect of a novel scaffold, oxaza spiroquinone
-
Here we first time report an unprecedented and unnatural six-membered 1,5-oxaza spiroquinone scaffold with structural novelty, a convenient and efficient synthetic route was developed for the synthesis of new 1,5-oxaza spiroquinone derivatives (1a-1r) in
- Venkanna, Arramshetti,Cho, Kyo Hee,Dhorma, Lama Prema,Kumar, Duddukuri Nandan,Hah, Jung Mi,Park, Hyeung-geun,Kim, Sun Yeou,Kim, Mi-hyun
-
-
Read Online
- A new charge-tagged proline-based organocatalyst for mechanistic studies using electrospray mass spectrometry
-
A new 4-hydroxy-L-proline derivative with a charged 1-ethylpyridinium-4- phenoxy substituent has been synthesized with the aim of facilitating mechanistic studies of proline-catalyzed reactions by ESI mass spectrometry. The charged residue ensures a stron
- Willms, J. Alexander,Beel, Rita,Schmidt, Martin L.,Mundt, Christian,Engeser, Marianne
-
-
Read Online
- The Catalytic Asymmetric Intermolecular Prins Reaction
-
Despite their significant potential, catalytic asymmetric reactions of olefins with formaldehyde are rare and metal-free approaches have not been previously disclosed. Here we describe an enantioselective intermolecular Prins reaction of styrenes and paraformaldehyde to form 1,3-dioxanes, using confined imino-imidodiphosphate (iIDP) Br?nsted acid catalysts. Isotope labeling experiments and computations suggest a concerted, highly asynchronous addition of an acid-activated formaldehyde oligomer to the olefin. The enantioenriched 1,3-dioxanes can be transformed into the corresponding optically active 1,3-diols, which are valuable synthetic building blocks.
- Diáz-Oviedo, C. David,Maji, Rajat,List, Benjamin
-
supporting information
p. 20598 - 20604
(2021/12/14)
-
- Concise and practical approach for the synthesis of honokiol, a neurotrophic agent
-
An improved method has been developed for the synthesis of honokiol using a readily available p-bromophenol as a precursor. The key step involved in this method is ortho-lithiation facilitated by methoxymethyl ether (MOM). Other important steps are ortho-allyl phenyl ether Claisen rearrangement and a Suzuki coupling for the construction of biaryls. This method does not require pre-functionalization of aromatic ring with bromide for the generation of arylboronic acid.
- Khan, P. Rasvan,Mujawar, Taufiqueahmed,Shankar, G.,Shekhar, P.,Subba Reddy, BV.,Subramanyam, Ravi
-
supporting information
(2020/08/06)
-
- Preparation method of 4-(4-hydroxyphenyl) cyclohexanone
-
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.
- -
-
Paragraph 0068-0071
(2019/08/01)
-
- SSAO INHIBITORS AND USES THEREOF
-
Described herein are compounds that are semicarbazide-sensitive amine oxidase (SSAO) inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in treating or preventing a liver disease or condition.
- -
-
Paragraph 00488
(2020/01/08)
-
- Highly hindered 2-(aryl-di-tert -butylsilyl)- N -methyl-imidazoles: A new tool for the aqueous 19F- and 18F-fluorination of biomolecule-based structures
-
A new class of silicon-based fluoride acceptors with a C-linked heterocycle as the leaving group was synthesized in one step from commercial chemicals, and linked to biomolecules. The resulting conjugates were efficiently 19F-fluorinated in aqu
- Tisseraud, Marion,Schulz, Jürgen,Vimont, Delphine,Berlande, Murielle,Fernandez, Philippe,Hermange, Philippe,Fouquet, Eric
-
supporting information
p. 5098 - 5101
(2018/05/26)
-
- NOVEL SPIROQUINONE DERIVATIVE COMPOUND, PRODUCTION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING NEUROLOGICAL DISORDERS WHICH CONTAINS SAME AS ACTIVE INGREDIENT
-
The present invention relates to a novel spiroquinone derivative compound, a production method thereof, and a pharmaceutical composition for preventing or treating neurological disorders which contains the compound as an active ingredient, and it has been
- -
-
Paragraph 0121; 0122
(2018/11/21)
-
- Wnt signal pathway inhibitor and use thereof
-
The invention relates to heterocyclic compounds with Wnt signal channel inhibition activity, particularly including compounds, pharmaceutically acceptable salts, various isotopes, various isomers or various crystal structures thereof having a structure represented by a general formula I (shown in the specification). By the compounds and a composition of the compounds, a Wnt signal channel can be effectively inhibited and diseases related to the Wnt signal channel can be treated or prevented.
- -
-
Paragraph 0047; 0084-0087
(2017/08/10)
-
- Total synthesis of [13C]2-, [13C]3-, and [13C]5-isotopomers of xanthohumol, the principal prenylflavonoid from hops
-
Xanthohumol [(E)-6′-methoxy-3′-(3-methylbuten-2-yl)-2′,4′,4″-trihydroxychalcone], he principal prenylated flavonoid from hops, has a complex bioactivity profile, and 13C-labeled isotopomers of this compound are of potential use as molecular probes and as analytical standards to study metabolism and mode of action. 1,3-[13C]2-Xanthohumol was prepared by an adaptation of the total synthesis of Khupse and Erhardt in 7 steps and 5.7% overall yield from phloroglucinol by a route incorporating a cascade Claisen-Cope rearrangement to install the 3′-prenyl moiety from a 5′-prenyl aryl ether and an aldol condensation between 1-[13C]-2′,4′-bis(benzyloxymethyloxy)-6′-methoxy-3′-(3-methylbuten-2-yl)acetophenone and 1′-[13C]-4-(methoxymethyloxy)benzaldehyde. The 13C-atom in the methyl ketone was derived from 1-[13C]-acetyl chloride while that in the aryl aldehyde was derived from [13C]-iodomethane. Tri- and penta-13C-labeled xanthohumols were similarly prepared by applying minor modifications to the route.
- Ellinwood, Duncan C.,El-Mansy, Mohamed F.,Plagmann, Layhna S.,Stevens, Jan F.,Maier, Claudia S.,Gombart, Adrian F.,Blakemore, Paul R.
-
p. 639 - 648
(2017/11/27)
-
- Development of Phenyl Cyclohexylcarboxamides as a Novel Class of Hsp90 C-terminal Inhibitors
-
Inhibition of the heat shock protein 90 (Hsp90) C-terminus represents a promising therapeutic strategy for the treatment of cancer. Novobiocin, a coumarin antibiotic, was the first Hsp90 C-terminal inhibitor identified, however, it manifested poor anti-proliferative activity (SKBr3, IC50≈700 μm). Subsequent structure–activity relationship (SAR) studies on novobiocin led to development of several analogues that exhibited improved anti-proliferative activity against several cancer cell lines. Recent studies demonstrate that the biphenyl core could be used in lieu of the coumarin ring system, which resulted in more efficacious analogues. In continuation of previous efforts, the work described herein has identified the phenyl cyclohexyl core as a novel scaffold for Hsp90 C-terminal inhibition. Structure–activity relationship (SAR) studies on this scaffold led to the development of compounds that manifest mid-nanomolar activity against SKBr3 and MCF-7 breast cancer cell lines through Hsp90 inhibition.
- Garg, Gaurav,Forsberg, Leah K.,Zhao, Huiping,Blagg, Brian S. J.
-
supporting information
p. 16574 - 16585
(2017/11/13)
-
- Polymerizable compound, polymerizable composition, and liquid crystal display element
-
Provided are: a polymerizable compound having a high polymerization reactivity, a high conversion rate and a high solubility in liquid crystal compositions; a polymerizable composition containing said compound; a liquid crystal composite prepared from sai
- -
-
Paragraph 0272; 0273; 0274
(2016/10/07)
-
- POLYMERIZABLE COMPOUND, POLYMERIZABLE COMPOSITION, AND LIQUID CRYSTAL DISPLAY ELEMENT
-
To provide a polymerizable compound having a high polymerizability, a high conversion ratio and a high solubility in a liquid crystal composition, a polymerizable composition containing the compound, a liquid crystal composite prepared from the compositio
- -
-
Paragraph 0301; 0303-0305
(2016/10/27)
-
- Exploration of the linkage elements of porcupine antagonists led to potent Wnt signaling pathway inhibitors
-
The Wnt signaling pathway is a pivotal developmental pathway. It operates through control of cellular functions such as proliferation, differentiation, migration and polarity. Aberrant Wnt signaling has been implicated in the formation and metastasis of tumors. Porcupine is a component of the Wnt signaling pathway. It is a member of the membrane-bound O-acyltransferase family of proteins. Porcupine catalyzes the palmitoylation of Wnt proteins, a process which is essential to their secretion and activity. Here we report a novel series of compounds obtained by a scaffold hybridization strategy from two known porcupine inhibitor classes. The leading compound 62 demonstrated subnanomolar (IC50 0.11 nM) inhibition of Wnt signaling in a paracrine cellular reporter gene assay. Compound 62 also potently inhibited Wnt secretion into culture medium, an indication of direct inhibition of the porcupine protein. Furthermore, compound 62 showed excellent chemical, plasma and liver microsomal stabilities. Collectively, these results strongly support further optimization of this novel scaffold to develop better Wnt pathway inhibitors.
- Dong, Yan,Li, Kehuang,Xu, Zhixiang,Ma, Haikuo,Zheng, Jiyue,Hu, Zhilin,He, Sudan,Wu, Yiyuan,Sun, Zhijian,Luo, Lusong,Li, Jiajun,Zhang, Hongjian,Zhang, Xiaohu
-
p. 6855 - 6868
(2015/11/11)
-
- Refrigerator
-
The present invention relates to a refrigerator, including: a refrigerating cycle having an evaporator (1a); a space for exchanging heat with the evaporator; a region for exchanging heat between the evaporator and the space; and a storage chamber and a door for defining the space, wherein at least one of the region, the storage chamber and the door has undergone at least one of a Kimchi lactic acid bacteria culture treatment and a Kimchi lactic acid bacteria culture exposure treatment.
- -
-
-
- Isolation, synthesis, and biological activity of biphenyl and m-terphenyl-type compounds from Dictyostelium cellular slime molds
-
From the fruiting bodies of Dictyostelium polycephalum, we obtained four aromatic compounds: dictyobiphenyl A (1) and B (2) and dictyoterphenyl A (3) and B (4). The synthesis of 1-4 was performed to confirm the structures and obtain sufficient material fo
- Kikuchi, Haruhisa,Matsuo, Yusuke,Katou, Yasuhiro,Kubohara, Yuzuru,Oshima, Yoshiteru
-
p. 8884 - 8889
(2012/10/29)
-
- NOVEL DIHYDROPYRIMIDIN-2(1H)-ONE COMPOUNDS AS S-NITROSOGLUTATHIONE REDUCTASE INHIBITORS
-
The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
- -
-
Page/Page column 141-142
(2011/04/24)
-
- Synthesis of 1,4-bis[2,2-bis(4-alkoxyphenyl)vinyl]benzenes and side chain modulation of their solid-state emission
-
Figure Presented. A series of 1,4-bis[2,2-bis(4-alkoxyphenyl)vinyl]benzene molecules with aggregation-induced emission (AIE) activity were synthesized. The conformations and packing arrangements of these molecules in the solid state can be adjusted by changing the side chains, which subsequently modulates their solid-state emission. The fluorescence quantum yield of 1e with the n-C 6H13 side chain in the solid state could reach up to 60.3% in the solid state.
- An, Peng,Shi, Zi-Fa,Dou, Wei,Cao, Xiao-Ping,Zhang, Hao-Li
-
supporting information; experimental part
p. 4364 - 4367
(2010/11/17)
-
- REVERSE TRANSCRIPTASE INHIBITORS
-
Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using t
- -
-
Page/Page column 122
(2009/07/10)
-
- Electron acceptors for nonlinear optical chromophores
-
Electron acceptor compounds, nonlinear optical chromophores made from the electron acceptor compounds, methods for making the electron acceptor compounds and nonlinear optical chromophores, lattices that include the nonlinear optical chromophores, and devices that include the nonlinear optical chromophores.
- -
-
Page/Page column 16
(2008/12/08)
-
- Syntheses of sterically hindered pyridinium phenoxides as model compounds in nonlinear optics
-
Noncentrosymmetric molecules with a π-conjugated system and, among them, push-pull molecules such as pyridinium phenoxide, are a promising new class of materials for applications in optoelectronics due to their nonlinear optical (NLO) properties. Modelling studies have indicated that an increase in the twist angle between the two aromatic rings leads to an enhancement of the NLO properties. In order to confirm this feature experimentally, it was necessary to prepare a series of new hindered pyridinium phenoxides. Their efficient syntheses by Suzuki cross-coupling reactions are described herein. Wiley-VCH Verlag GmbH & Co. KGaA, 2006.
- Diemer, Vincent,Chaumeil, Helene,Defoin, Albert,Fort, Alain,Boeglin, Alex,Carre, Christiane
-
p. 2727 - 2738
(2007/10/03)
-
- Synthesis of [125I]-, [2H]-, and [ 3H]-labeled 3-iodothyronamine (T1AM)
-
3-Iodothyronamine (T1AM) is a novel metabolite of thyroid hormone. In HEK-293 cells expressing an orphan G-protein coupled receptor, the trace amine receptor, T1AM, potently increased cAMP accumulation. In mice, T1AM rapid
- Miyakawa, Motonori,Scanlan, Thomas
-
p. 891 - 902
(2007/10/03)
-
- Trace amine-associated receptor agonists: Synthesis and evaluation of thyronamines and related analogues
-
We have previously shown that several thyronamines, decarboxylated and deiodinated metabolites of the thyroid hormone, potently activate an orphan G protein-coupled receptor in vitro (TAAR1) and induced hypothermia in vivo on a rapid time scale [Scanlan, T. S.; Suchland, K. L.; Hart, M. E.; Chiellini, G.; Huang, Y.; Kruzich, P. J.; Frascarelli, S.; Crossley, D. A.; Bunzow, J. R.; Ronca-Testoni, S.; Lin, E. T.; Hatton, D.; Zucchi, R.; Grandy, D. K. 3-Iodothyronamine is an endogenous and rapid-acting derivative of thyroid hormone. Nat. Med. 2004, 10 (6), 638-642]. Herein, we report the synthesis of these thyronamines. Additionally, a large number of thyroamine derivatives were synthesized in an effort to understand the molecular basis of TAAR1 activation and hypothermia induction. Several derivatives were found to potently activate both rTAAR1 and mTAAR1 in vitro (compounds 77, 85, 91, and 92). When administered to mice at a 50 mg/kg dose, these derivatives all induced significant hypothermia within 60 min and exhibited a hypothermic induction profile analogous to 3-iodothyronamine (1, T1AM) except 91, which proved to be more efficacious. On the basis of this result, a dose-dependent profile for 91 was generated and an ED50 of 30 μmol/kg was calculated. Compound 91 proved to be more potent than T1AM for TAAR1 activation and exhibits increased potency and efficacy for hypothermia induction. These data further strengthen the pharmacological correlation linking TAAR1 activation by thyronamines and hypothermia induction in mice.
- Hart, Matthew E.,Suchland, Katherine L.,Miyakawa, Motonori,Bunzow, James R.,Grandy, David K.,Scanlan, Thomas S.
-
p. 1101 - 1112
(2007/10/03)
-
- A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies
-
A strategy to obtain a fully orthogonal estrogen-receptor-based gene switch responsive to molecules with acceptable pharmacological properties is presented. From a series of tetrahydrofluorenones active on the wild-type estrogen receptor (ER) an inactive
- Kinzel, Olaf,Fattori, Daniela,Muraglia, Ester,Gallinari, Paola,Nardi, Maria Chiara,Paolini, Chantal,Roscilli, Giuseppe,Toniatti, Carlo,Gonzalez Paz, Odalys,Laufer, Ralph,Lahm, Armin,Tramontano, Anna,Cortese, Riccardo,De Francesco, Raffaele,Ciliberto, Gennaro,Koch, Uwe
-
p. 5404 - 5407
(2007/10/03)
-
- Diphenylimidazopyrimidine and -imidazole amines as inhibitors of beta-secretase
-
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated β-amyloid deposits or β-amyloid levels in a patient.
- -
-
Page/Page column 21
(2008/06/13)
-
- CHEMICAL COMPOUNDS
-
The present invention relates to novel compounds with a variety of therapeutic uses, more particularly novel substituted cyclic alkylidene compounds that are particularly useful for selective estrogen receptor modulation.
- -
-
Page/Page column 82
(2008/06/13)
-
- Synthesis of 4-[N-methyl-4-pyridinio]-phenolate (POMP) and negative solvatochromism of this model molecule in view of nonlinear optical applications
-
4-[N-Methyl-4-pyridinio]-phenolate or [4-(phenyloxido)-N-methylpyridinium, POMP] has been synthesized via Suzuki cross-coupling reaction. POMP undergoes a strong negative solvatochromism (blue shift) as the solvent polarity increases and behaves qualitati
- Diemer, Vincent,Chaumeil, Hélène,Defoin, Albert,Jacques, Patrice,Carré, Christiane
-
p. 4737 - 4740
(2007/10/03)
-
- NOVEL COMPOUNDS
-
The present invention relates to novel compounds with a variety of therapeutic uses, more particularly novel prodrugs that are particularly useful for delivering a parent compound for selective estrogen receptor modulation.
- -
-
Page/Page column 44-47
(2010/02/11)
-
- PERFLUOROALLYLOXY COMPOUND AND LIQUID CRYSTAL COMPOSITION CONTAINING THE COMPOUND
-
A novel perfluoroallyloxy compound represented by general formula (I) and a liquid crystal composition containing the compound are disclosed. The perfluoroallyloxy compound is useful as a liquid crystal material.
- -
-
-
- SUBSTITUTED BENZOPYRANS AS SELECTIVE ESTROGEN RECEPTOR-BETA AGONISTS
-
The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof and processes for the preparation of the same. The compounds of the present invention are useful as Estrogen Receptor ? agonists. Such agonists are useful for the treating Estrogen Receptor ? mediated diseases such as prostate cancer or BPH.
- -
-
Page 8; 14-15
(2010/02/09)
-
- ARYL SULFAMATE DERIVATIVES
-
The present invention provides an aryl sulfamate derivative represented by Formula (I) (wherein Rr and Rs, which may be the same or different, each represent a hydrogen atom or lower alkyl, R1, R2, R3
- -
-
-
- Synthesis and structure-activity relationship for new series of 4-phenoxyquinoline derivatives as specific inhibitors of platelet-derived growth factor receptor tyrosine kinase
-
We discovered a new series of 4-phenoxyquinoline derivatives as potent and selective inhibitors of the platelet-derived growth factor receptor (PDGFr) tyrosine kinase. We researched the highly potent and selective inhibitors on the basis of both PDGFr and epidermal growth factor receptor (EGFr) inhibitory activity. First, we found a compound, Ki6783 (1), which inhibited PDGFr autophosphorylation at 0.13 μM, but it did not inhibit EGFr autophosphorylation at 100 μM. After extensive explorations, we found the two desired compounds, Ki6896 (2) and Ki6945 (3), which are substituted by benzoyl and benzamide at the 4-position of the phenoxy group on 4-phenoxyquinoline, respectively. These inhibitory activities were 0.31 and 0.050 μM, respectively, but neither of them inhibited EGFr autophosphorylation at 100 μM. We further investigated the profile of both compounds toward various tyrosine and serine/threonine kinases. The three compounds specifically inhibited PDGFr rather than the other kinases.
- Kubo, Kazuo,Ohyama, Shin-Ichi,Shimizu, Toshiyuki,Takami, Atsuya,Murooka, Hideko,Nishitoba, Tsuyoshi,Kato, Shinichiro,Yagi, Mikio,Kobayashi, Yoshiko,Iinuma, Noriko,Isoe, Toshiyuki,Nakamura, Kazuhide,Iijima, Hiroshi,Osawa, Tatsushi,Izawa, Toshio
-
p. 5117 - 5133
(2007/10/03)
-
- Biphenyl derivatives substituted by an aromatic or heteroaromatic radical and pharamaceutical and cosmetic compositions containing same
-
“Biphenyl derivatives substituted with an aromatic or heteroaromatic radical, and pharmaceutical and cosmetic compositions containing them” in which: Ar represents an aromatic or a heteroaromatic radical optionally substituted, in particular, with an alkyl or a carboxyl group, R2and R3represent, in particular, H or alkyl, or R2and R3, taken together, form a 5- or 6-membered ring, R4and R5represent, in particular, H or halogen, R6represents, in particular, H or lower alkyl, and the salts of the compounds of formula (I). These compounds can be used in particular in the treatment of dermatological complaints associated with a keratinization disorder, and for combating ageing of the skin.
- -
-
-
- Anilide derivative, production and use thereof
-
This invention is to provide a compound of the formula: wherein R1is an optionally substituted 5- to 6-membered ring; the ring A is an optionally substituted 6- to 7-membered ring; the ring B is an optionally substituted benzene ring; n is an integer of 1 or 2; Z is a chemical bond or a divalent group; R2is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, (2) an optionally substituted nitrogen-containing heterocyclic ring group which may contain a sulfur atom or an oxygen atom as ring constituting atoms and wherein a nitrogen atom may form a quaternary ammonium, (3) a group binding through a sulfur atom or (4) a group of the formula: ?wherein k is 0 or 1, and when k is 0, a phosphorus atom may form a phosphonium; and R5and R6are independently an optionally substituted hydrocarbon group, an optionally substituted hydroxy group or an optionally substituted amino group, and R5and R6may bind to each other to form a cyclic group together with the adjacent phosphorus atom, or a salt thereof , which is useful for antagonizing CCR5 and also for the prevention and treatment of infectious disease of HIV.
- -
-
-
- Triaromatic compounds and pharmaceutical/cosmetic compositions comprised thereof
-
Novel pharmaceutically/cosmetically-active triaromatic compounds have the structural formula (I): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
- -
-
-
- NOVEL HETEROCYCLIC COMPOUNDS HAVING PLATELET AGGREGATION INHIBITORY EFFECTS
-
Disclosed are a compound represented by the following formula (I) and pharmacologically acceptable salt and solvate thereof having inhibitory activity against platelet aggregation: ???wherein A represents the following formula (II), (III), or (IV): A phar
- -
-
-
- Facile methods for the direct conversions of aryl acetates into the corresponding methoxymethyl ethers or silyl ethers
-
Direct conversion of aryl acetates into aryl methoxymethyl ethers or aryl trialkylsilyl ethers was readily accomplished by treatment with methoxymethyl bromide or trialkylsilyl trifluoromethanesulfonate, respectively, in the presence of sodium methoxide.
- Oriyama, Takeshi,Noda, Kojiro,Sugawara, Satomi
-
p. 2217 - 2223
(2007/10/03)
-
- An asymmetric synthesis of L-[3-13C]phenylalanine and L-[3- 13C]tyrosine from [13C]carbon monoxide
-
L-[3-13C]Phenylalanine and L-[3-13C]tyrosine were synthesized. [α- 13C]Benzyl bromides were prepared from [13C]carbon monoxide via the palladium-catalyzed carboalkoxylation of aryl halides. The asymmetric carbon corresponding to the 2-position in phenylalanine was introduced by the diastereoselective alkylation of Dellaria's oxazinone with [α-13C]benzyl bromides. Finally, ethanolysis, deprotection, hydrogenolysis and acid hydrolysis of the resulting alkylated oxazinones gave L-[3- 13C]phenylalanine and L-[3-13C]tyrosine in high optical purity.
- Takatori, Kazuhiko,Nishihara, Mikiko,Nishiyama, Yukie,Kajiwara, Masahiro
-
p. 15861 - 15869
(2007/10/03)
-
- Azoxy compound
-
An azoxy compound represented by the following general formula STR1 wherein R1 denotes a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkoxy group, a lower alkoxy-lower alkoxy group or a group of the formula X1 --C C--CH
- -
-
-
- Total Synthesis of Grossularines-1 and -2
-
The first total syntheses of grossularines-1 (1a) and -2 (1b) have been completed.The cross-coupling reaction between ethyl 3-iodoindole-2-carboxylate (6) and the directed metalation-derived imidazole 9b gave the ethyl 3-(5-imidazolyl)indole-2-carboxylate 11b.Hydrolysis of the ester group of 11b, followed by Curtius rearrangement, yielded the 2-isocyanatoindole 13b.The thermal electrocyclic reaction of 13b was carried out to provide the desired tetracyclic pyridoindole ring system 14b, which was converted into the triflate 15b.The three-component cross-coupling reaction of the triflate 15b, carbon monoxide, and p-(OMOM)phenylboronic acid (17) followed by hydrolysis gave glossularine-2 (1b) in low yield.In addition, the palladium-catalyzed carbonylation of the triflate 15b afforded the N-deprotected methyl ester 19a or the methyl ester 19b depending on the amounts of triethylamine used.Compound 19a was treated with either p-(OMOM)phenyllithium or 3-(N-TIPS)indolyllithium to obtain grossularine-2 (1b) and grossularine-1 (1a) (37percent), respectively.By contrast, when 19b was treated with the same aryllithium reagents, grossularine-2 (1b) (51percent) and grossularine-1 (1a) (63percent) were produced, respectively.
- Choshi, Tominari,Yamada, Shiho,Sugino, Eiichi,Kuwada, Takeshi,Hibino, Satoshi
-
p. 5899 - 5904
(2007/10/03)
-
- Syntheses of nitro-substituted aryl diazirines. An entry to chromogenic carbene precursors for photoaffinity labeling
-
3-Phenyl-3-trifluoromethyl-diazirine derivatives with nitro and alkoxy substituents on their aromatic ring have been synthesized as carbene precursors for chromogenic detection of photolabeled products. Photolysis of the diazirines in methanol or cyclohex
- Hatanaka,Hashimoto,Nakayama,Kanaoka
-
p. 826 - 831
(2007/10/02)
-
- Organosilylalkylaromatic compounds
-
The present invention relates to compounds of the formula STR1 in which Y represents an organosilicon radical; R" represents a divalent radical which connects the radical Y to the benzene ring via a chain of at least three atoms; X represents a radical of the formula --COOH, --CN, --CHO, --NH2 or --OH, in which it is possible to block the hydroxyl group with a protecting group; Z represents the same or different substituents in the 2-, 3-, 5- or 6-position to the radical X, preferably hydrogen or halogen atoms; and p represents a value of 0 to 4; and the use of these and related compounds in the preparation of compounds having liquid-crystalline properties.
- -
-
-
- Cyclosiloxanes containing mesogenic side groups
-
The present invention relates to cyclic siloxanes which have at least one group of formula (1) bonded to a silicon atom in which x is an integer having a value of at least 2, preferably having a value of from 2 to 10, R" is a chemical bond or a divalent r
- -
-
-
- Synthesis and Carbon-13 Nuclear Magnetic Resonance Assignments of Xenognosin
-
Xenognosin (1) is a modified flavonoid isolated from gum tragacanth, and it stands as the first natural host recognition substance for parasitic angiosperms.Xenognosin (1) was synthesized by converting umbelliferone (2) to the key aldehyde 6 which was tre
- El-Feraly, Farouk S.,Hufford, Charles D.
-
p. 1527 - 1530
(2007/10/02)
-