- Controlling the Spatial Organization of Liquid Crystalline Nanoparticles by Composition of the Organic Grafting Layer
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Understanding how the spatial ordering of liquid crystalline nanoparticles can be controlled by different factors is of great importance in the further development of their photonic applications. In this paper, we report a new key parameter to control the mesogenic behavior of gold nanoparticles modified by rodlike thiols. An efficient method to control the spatial arrangement of hybrid nanoparticles in a condensed state is developed by changing the composition of the mesogenic grafting layer on the surface of the nanoparticles. The composition can be tuned by different conditions of the ligand exchange reaction. The thermal and optical behavior of the mesogenic and promesogenic ligands were investigated by using differential scanning calorimetry (DSC) and hot-stage polarized optical microscopy. The chemical structure of the synthesized hybrid nanoparticles was characterized by 1HNMR spectroscopy, thermogravimetric analysis (TGA), XPS, and elemental analysis, whereas the superstructures were examined by small-angle X-ray diffraction (SAXSRD) analysis. Structural studies showed that the organic sublayer made of mesogenic ligands is denser with an increasing the average ligand number, thereby separating the nanoparticles in the liquid crystalline phases, which changes the parameters of these phases. Softening nanocrystalline gold: An efficient method to control the spatial arrangement of liquid crystalline gold nanoparticles was developed by changing the composition of the mesogenic grafting layer. Structural studies showed that the organic sublayer is more dense with increasing average ligand number, thereby separating the nanoparticles in the liquid crystalline phases, which changes the parameters of these phases (see figure).
- W?jcik, Micha? M.,Olesińska, Magdalena,Sawczyk, Micha?,Mieczkowski, J?zef,G?recka, Ewa
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Read Online
- Novel bifunctional hybrid small molecule scavengers for mitigating nerve agents toxicity
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The antidotal treatment of organophosphates (OP) nerve agents (NA) poisoning is based on anticholinergics (e.g. atropine) combined with oxime reactivators (e.g. 2PAM) of acetylcholinesterase (AChE). This treatment is symptomatic and does not degrade the OP. New small-molecule OP scavengers were developed as bifunctional hybrids. Their molecular design was based on combining a nucleophile that directly degrades OP with a moiety that reactivates OP-inhibited AChE. The OP degrading moiety is either benzhydroxamic acid (BHA) or 4-pyridinehydroxamic acid (4PHA) coupled via [sbnd](CH2)n[sbnd], (n = 1 or 3) to 2PAM. Three newly synthesized oxime-hydroxamate hybrids: 2PAMPr4PHA, 2PAMMeBHA and 2,4-DiPAMMeBHA were found to detoxify sarin, cyclosarin and soman in solution at 3–10-fold faster rate than 2PAM and to reactivate OP-AChE in vitro. 2PAMPr4PHA displayed 18-fold faster reactivation than 2-PAM of cyclosarin-inhibited HuAChE (kr = 3.6 × 102 vs. 0.2 × 102 M?1min?1, respectively, 37 °C). These hybrids inhibited AChE reversibly, IC50 = 16–48 μM, thereby decreasing the inhibition rates by OPs. The LD50 (im) of 2PAMPr4PHA, 2PAMMeBHA and 2,4DiPAMMeBHA are >568, 508 and >506 μmol/kg in rats and 144, 203 and >506 μmol/kg in guinea pigs. The rate of blood ChE recovery by the hybrids administered either pre- or post-exposure to 0.8xLD50 sarin was comparable or faster than 2PAM. Antidotal efficacy of 2PAMPr4PHA, 2PAMMeBHA and 2,4DiPAMMeBHA administered with atropine, as pre-treatment to sarin in rats (im), yielded protection ratios (PR) 11.6, 11.5 and 4.7, respectively, vs. 5.5 with 2PAM. Post-treatment against various OPs in rats and guinea-pigs yielded PRs higher or similar to that of 2 PAM. Our in vivo data indicates that some hybrids may serve as efficient small molecule scavengers for mitigating the toxicity of OP NAs.
- Amitai, Gabriel,Gez, Rellie,Raveh, Lily,Bar-Ner, Nira,Grauer, Ettie,Chapman, Shira
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Read Online
- Pd-catalyzed sp-sp3cross-coupling of benzyl bromides using lithium acetylides
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Organolithium-based cross-coupling reactions have emerged as an indispensable method to construct C-C bonds. These transformations have proven particularly useful for the direct and fast coupling of various organolithium reagents (sp, sp2, and sp3) with aromatic (pseudo) halides (sp2). Here we present an efficient method for the cross-coupling of benzyl bromides (sp3) with lithium acetylides (sp). The reaction proceeds within 10 min at room temperature and can be performed in the presence of organolithium-sensitive functional groups such as esters, nitriles, amides and boronic esters. The potential application of the methodology is demonstrated in the preparation of key intermediates used in pharmaceuticals, chemical biology and natural products.
- Buter, Jeffrey,Doze, Anna M.,Feringa, Ben L.,Mondal, Anirban,Visser, Paco
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supporting information
p. 7529 - 7532
(2021/08/05)
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- From Kinase Inhibitors to Multitarget Ligands as Powerful Drug Leads for Alzheimer's Disease using Protein-Templated Synthesis
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Multitarget directed ligands (MTDLs) are arising as promising tools to tackle complex diseases. The main goal of this work is to create powerful modulating agents for neurodegenerative disorders. To achieve this aim, we have combined fragments that inhibi
- Nozal, Vanesa,García-Rubia, Alfonso,Cuevas, Eva P.,Pérez, Concepción,Tosat-Bitrián, Carlota,Bartolomé, Fernando,Carro, Eva,Ramírez, David,Palomo, Valle,Martínez, Ana
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supporting information
p. 19344 - 19354
(2021/07/28)
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- 1, 3-di-substituted-4-amino pyrazolopyrimidine compound, preparation method thereof and application of compound
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The invention relates to a 1, 3-di-substituted-4-amino pyrazolopyrimidine compound, a preparation method thereof and an application of the compound. The compound is provided with a structure as shownin a formula I. The invention further relates to a preparation method of the compound with the structure as shown in the formula I and a medicine composition. The invention further provides an application of the compound and pharmaceutically acceptable salt thereof to preparation of MCL (mantle cell lymphoma) resistance medicines.
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Paragraph 0103; 0118-0119
(2019/03/08)
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- Revefenacin intermediate, preparation method thereof and preparation method of revefenacin
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The invention relates to the field of pharmaceutical synthesis, in particular to a revefenacin key intermediate (II), and also relates to a preparation method of the intermediate (II) and a method forpreparing revefenacin as shown in a formula (I) through the intermediate (II). The intermediate (II) is prepared from a compound (IV) and a compound (V) which are subjected to an amidation reaction.The revefenacin can be obtained from the intermediate (II) through a substitution reaction. A synthesis route is mild in condition, the conversion rate and selectivity are high, the reaction yield andthe reaction efficiency are high, energy consumption is low, post-treatment is convenient, reaction operation is easy and convenient, and the method for preparing the revefenacin shown in the formula(I) through the intermediate (II) is more suitable for industrial production.
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Paragraph 0049; 0051
(2019/12/25)
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- ONE-BEAD-TWO-COMPOUND MACROCYCLIC LIBRARY AND METHODS OF PREPARATION AND USE
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A one-bead-two-compound combinatorial synthesis technique provides libraries of macrocyclic peptidomimetic compounds and compositions with use as ligands for the Ephrin type-A receptor 2 (EphA2). The one-bead-two-compound technique and libraries of macrocyclic compounds are useful as research tools in drug discovery and/or to treat or prevent a range of diseases or disorders.
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Paragraph 0156; 0157
(2018/11/02)
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- Discovery of novel 5-methyl-1H-pyrazole derivatives as potential antiprostate cancer agents: Design, synthesis, molecular modeling, and biological evaluation
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Androgen receptor (AR) signaling functions as a core driving force for the progression of prostate cancer (PCa), and AR has been proved to be an effective therapeutic target even for castration-resistant prostate cancer (CRPC). Herein, structural modification via a fragments splicing strategy was performed based on two lead compounds T3 and 10e, leading to the discovery of a series of 5-methyl-1H-pyrazole derivatives. AR reporter gene assay revealed compounds A13 and A14 as potent AR antagonists. Some of the compounds in this series inhibited growth of PCa LNCaP cells more efficiently than enzalutamide. A13 and A14 also showed improved metabolic stability compared with 10e in human liver microsomes.
- Zhang, Daoguang,Asnake, Solomon,Zhang, Jingya,Olsson, Per-Erik,Zhao, Guisen
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p. 1113 - 1124
(2018/03/05)
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- 5-methyl-1H-pyrazole derivative, preparation method and applications thereof
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The invention discloses a 5-methyl-1H-pyrazole derivative, a preparation method and applications thereof, wherein the compound has a structure represented by a general formula (I). The invention further provides the preparation method and the applications
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Paragraph 0066
(2018/05/01)
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- 1. 3 - Benzoxazine - 2, 4 (3 H) - dione derivatives and their synthesis and use (by machine translation)
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The invention relates to a acetylcholine esterase with phosphodiesterase V enzyme inhibition benzoxazine dione derivative and its synthetic method and use, and in particular relates to the structure of the general formula (I) of 1, 3 benzoxazine - 2, 4 (3 H) - dione derivatives, R1 , R2 , R3 , R4 , R5 , R6 , R7 , R8 And R9 The specification of the existing limited to. This invention refers to these compound structure and synthetic method and in vitro acetylcholine esterase with phosphodiesterase V inhibiting activity, can be further developed into new drugs for treating Alzheimer's disease. (by machine translation)
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Paragraph 0020; 0026; 0027
(2018/10/19)
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- [...] aromatic amines acetylcholine esterase inhibitor synthesis and use (by machine translation)
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The present invention provides a formula for the (I) or (II) [...] aromatic amines of the acetylcholine esterase inhibitor and its pharmaceutically acceptable salt or a stereoisomer thereof, a process for their preparation and its in the preparation of acetylcholine esterase inhibitors and treatment of Alzheimer's disease and/or myasthenic application of the medicament, type definition of each group in the specification. The invention of aromatic amine derivatives as [...] of acetylcholine esterase inhibitors with micromolar level to nanomolar inhibiting activity, has further developed into an anti-Alzheimer's disease possibility of drug. (by machine translation)
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Paragraph 0046; 0048
(2018/10/19)
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- One-Bead-Two-Compound Thioether Bridged Macrocyclic γ-AApeptide Screening Library against EphA2
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Identification of molecular ligands that recognize peptides or proteins is significant but poses a fundamental challenge in chemical biology and biomedical sciences. Development of cyclic peptidomimetic library is scarce, and thus discovery of cyclic peptidomimetic ligands for protein targets is rare. Herein we report the unprecedented one-bead-two-compound (OBTC) combinatorial library based on a novel class of the macrocyclic peptidomimetics γ-AApeptides. In the library, we utilized the coding peptide tags synthesized with Dde-protected α-amino acids, which were orthogonal to solid phase synthesis of γ-AApeptides. Employing the thioether linkage, the desired macrocyclic γ-AApeptides were found to be effective for ligand identification. Screening the library against the receptor tyrosine kinase EphA2 led to the discovery of one lead compound that tightly bound to EphA2 (Kd = 81 nM) and potently antagonized EphA2-mediated signaling. This new approach of macrocyclic peptidomimetic library may lead to a novel platform for biomacromolecular surface recognition and function modulation.
- Shi, Yan,Challa, Sridevi,Sang, Peng,She, Fengyu,Li, Chunpu,Gray, Geoffrey M.,Nimmagadda, Alekhya,Teng, Peng,Odom, Timothy,Wang, Yan,Van Der Vaart, Arjan,Li, Qi,Cai, Jianfeng
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p. 9290 - 9298
(2017/11/30)
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- Liquid-Crystalline Elastomers with Gold Nanoparticle Cross-Linkers
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Embedding nanoparticles in a responsive polymer matrix is a formidable way to fabricate hybrid materials with predesigned properties and prospective applications in actuators, mechanically tunable optical elements, and electroclinic films. However, achieving chemical compatibility between nanoparticles and organic matter is not trivial and often results in disordered structures. Herein, it is shown that using nanoparticles as exclusive cross-linkers in the preparation of liquid-crystalline polymers can yield long-range-ordered liquid-crystalline elastomers with high loadings of well-dispersed nanoparticles, as confirmed by small-angle XRD measurements. Moreover, the strategy of incorporating NPs as cross-linking units does not result in disruption of mechanical properties of the polymer, and this phenomenon was explained by the means of all-atom molecular dynamics simulations. Such materials can exhibit switchable behavior under thermal stimulus with stability spanning over multiple heating/cooling cycles. The presented strategy has proven to be a promising approach for the preparation of new types of hybrid liquid-crystalline elastomers that can be of value for future photonic applications.
- Wójcik, Micha? M.,Wróbel, Jaros?aw,Jańczuk, Zuzanna Z.,Mieczkowski, Józef,Górecka, Ewa,Choi, Joonmyung,Cho, Maenghyo,Pociecha, Damian
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supporting information
p. 8912 - 8920
(2017/07/11)
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- Fused imidazoles as potential chemical scaffolds for inhibition of heat shock protein 70 and induction of apoptosis. Synthesis and biological evaluation of phenanthro[9,10-d] imidazoles and imidazo[4,5-f] [1,10]phenanthrolines
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The imidazole ring is widespread in biologically active compounds, and hence imidazole-containing scaffolds are useful starting points for drug discovery programmes. We report the synthesis of a series of novel imidazole-containing compounds fused with either phenanthrene or phenanthroline, which show enhanced growth inhibitory potency against human colon, breast and melanoma cancer cell lines, as well as evidence of inhibition of the molecular chaperone heat shock protein 70 (Hsp70) pathway in cells, as shown by depletion of downstream oncogenic client proteins of the Hsp90 chaperone pathway, and induction of apoptosis.
- Patel, Alpa,Sharp, Swee Y.,Hall, Katelan,Lewis, William,Stevens, Malcolm F.G.,Workman, Paul,Moody, Christopher J.
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p. 3889 - 3905
(2016/05/19)
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- Nickel(0)/NaHMDS adduct-mediated intramolecular alkylation of unactivated arenes via a homolytic aromatic substitution mechanism
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A variety of polycycles can be synthesized via an intramolecular alkylation cyclization promoted by Ni(PPh3)4 and NaHMDS. Mechanistic investigations support the catalytic nature of Ni0 in the course of TEMPO scavenging experiments and its association with the substrate and NaHMDS to form an adduct by DOSY NMR.
- Beaulieu, Louis-Philippe B.,Roman, Daniela Sustac,Vallee, Frederic,Charette, Andre B.
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supporting information; experimental part
p. 8249 - 8251
(2012/09/07)
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- MICROSOMAL PROSTAGLANDIN E SYNTHASE-1 (MPGES1) INHIBITORS
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A compound of formula (I): as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising the compound. The compound is useful for the treatment of disorder selected from inflammatory diseases, nociceptive pain, auto-imm
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Page/Page column 91
(2011/04/14)
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- Synthesis of aromatic oxazolyl- and carboxyl-functionalized polymers: Atom transfer radical polymerization of styrene initiated by 2-[(4-bromomethyl) phenyl]-4,5-dihydro-4,4-dimethyloxazole
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The synthesis of a new compound, 2-[(4-bromomethyl)phenyl]-4,5-dihydro-4,4- dimethyloxazole (1), and its utility in the synthesis of oxazoline- functionalized polystyrene by atom transfer radical polymerization (ATRP) methods are described. Aromatic oxazo
- Summers, Gabriel J.,Maseko, Rejoice B.,Beebeejaun, B. M. Parveen,Summers, Carol A.
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experimental part
p. 2601 - 2614
(2012/03/27)
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- Synthesis and in Vitro Cytotoxic Activity of Compounds with Pro-Apoptotic Potential
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In our search for new anticancer therapies, some compounds synthesized in our lab were selected and their potential cytotoxic activity was evaluated in vitro against two cancer cells lines including a solid tumor (UACC-62, melanoma) and a human lymphoma (
- Soares, Giselle Apicela,De Oliveira, Renata Barbosa,De Andrade, Saulo Fernandes,Alves, Ricardo Jose,Zani, Carlos Leomar,De Souza-Fagundes, Elaine Maria
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experimental part
p. 12 - 26
(2010/05/18)
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- Tripodal tris-tacn and tris-dpa platforms for assembling phosphate-templated trimetallic centers
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Multidentate tripodal ligands, N(CH2-m-C6H 4-CH2tacn)3 (L1) and N(CH2-o-C 6H4-CH2N(CH2py)2) 3 (L2), have been devised for assembling high-nuclearity metal clusters. By using the same tripodal platform with different ligand appendages, either triazacyclononanes or dipicolylamines, and functionalizing either the ortho or the meta positions on the tris(xylyl) linker arms, discrete trimetal phosphate units of relevance to phosphate-metabolizing trimetallic centers in biology were prepared. Four such compounds, [(CuIICl) 3(HPO4)L1](PF6) (1), [(CuIICl) 3(HAsO4)L1](PF6) (2), Na2[Mn III6MnII2(H2O) 2(HPO4)6(PO4)4(L1) 2] (3), and [CoII3(H2PO 4)Cl2(MeCN)L2](PF6)3 (4), all containing three metal centers bound to a central phosphate or arsenate unit bridging oxygen atoms, have been synthesized and structurally characterized. These results demonstrate the propensity of this novel tripodal ligand platform, in the presence of phosphate or arsenate, to assemble {M3(EO 4)} units and thus structurally mimic trimetallic active sites of proteins involved in phosphate metabolism. Reactivity studies reveal that the tricopper complex 1 is more efficient than monocopper analogues in catalyzing the hydrolysis of 4-nitrophenyl phosphate.
- Cao, Rui,Mueller, Peter,Lippard, Stephen J.
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supporting information; experimental part
p. 17366 - 17369
(2011/02/23)
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- Synthesis of novel tetrahydrofuran-epichlorohydrin [Poly(THF-b-ECH)] macromonomeric peroxy initiators by cationic copolymerization and the quantum chemically investigation of initiation system effects
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Cationic polymerization of tetrahydrofuran (THF) and epichlorohydrin (ECH) was performed with peroxy initiators synthesized from bis (4,4′- bromomethyl benzoyl peroxide (BBP) or bromomethyl benzoyl t-butyl peroxy ester (t-BuBP) and AgSbF6 or Zn
- Misir, Murat,Ozturk, Temel,Emirik, Mustafa,Yilmaz, Sevil S.
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scheme or table
p. 2896 - 2909
(2011/03/18)
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- NOVEL BIFUNCTIONAL COMPOUNDS WHICH INHIBIT PROTEIN KINASES AND HISTONE DEACETYLASES
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The present invention relates to a bifunctional compound of formula I or its pharmaceutically acceptable salts or solvates A-L-B (I) wherein A is a histone deacetylase (HDAC) inhibitory moiety, L is a single bond or a linker group and B is a protein kinase inhibitory moiety. The bifunctional compound according to formula (I) is useful for the treatment of malignant and non-malignant neoplasia and diseases related to abnormal cell growth
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Page/Page column 108-109
(2009/06/27)
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- Liquid-crystalline phases made of gold nanoparticles
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Spontaneous formation of smectic and columnar structures was observed when spherical gold nanoparticles were functionalized with mesogenic thiols (see layered structure and X-ray pattern of a sample in smectic phase). The particle ordering is stimulated b
- Wojcik, Michal,Lewandowski, Wiktor,Matraszek, Joanna,Mieczkowski, Jozef,Borysiuk, Jolanta,Pociecha, Damian,Gorecka, Ewa
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supporting information; experimental part
p. 5167 - 5169
(2009/12/08)
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- N-benzyl substituted pyridyl porphyrin compounds and methods of use thereof
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The present invention relates to N-Benzyl-Substituted Pyridyl Porphyrin Compounds, compositions comprising an effective amount of an N-Benzyl-Substituted Pyridyl Porphyrin Compound and methods for treating or preventing injury due to exposure to a reactiv
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Page/Page column 31
(2010/11/26)
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- THIAZOLE DERIVATIVE
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(Wherein n is an integer of from 0 to 3; R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, or a substituted or unsubstituted aromatic heterocyclic grou
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Page/Page column 105; 114
(2010/11/23)
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- Further optimization of sulfonamide analogs as EP1 receptor antagonists: Synthesis and evaluation of bioisosteres for the carboxylic acid group
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4-{[2-[(2-Furylsulfonyl)(isobutyl)amino]-5-(trifluoromethyl)phenoxy]methyl}benzoic acid analogs 2a and b and a series of the acid analogs, in which the carboxylic acid residue of 2b was replaced with various kinds of carboxylic acid bioisosteres, were synthesized and evaluated as EP1 receptor antagonists. Compound 2b and its monocyclic acid analogs, in which the carboxylic acid residue of 2b was replaced with monocyclic acid bioisosteres, were found to show potent EP1 receptor antagonist activity. Optimization of the linker Y between the phenyl moiety and the carboxylic acid residue of 2b was also carried out (Table 5). Compounds 2b and 16 and 17 possessing conformationally restricted linker Y were found to show the most optimized potency among the tested compounds. Cytochrome P450 inhibition of optimized compounds was also investigated. Details of the structure-activity relationship study are presented.
- Naganawa, Atsushi,Matsui, Toshiaki,Ima, Masaki,Saito, Tetsuji,Murota, Masayuki,Aratani, Yoshiyuki,Kijima, Hideomi,Yamamoto, Hiroshi,Maruyama, Takayuki,Ohuchida, Shuichi,Nakai, Hisao,Toda, Masaaki
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p. 7121 - 7137
(2007/10/03)
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- Therapeutic uses of tri-aryl acid derivatives
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The use of triaryl acid derivatives of formula (I) and their pharmaceutical compositions as PPAR ligand receptor binders. The PPAR ligand receptor binders of this invention are useful as agonists or antagonists of the PPAR receptor.
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Page/Page column 223-224
(2010/10/20)
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- Novel inhibitor compounds specific of secreted non-pancreatic human a2phospholipase of group II
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The present invention relates to a compound of the following formula (I) and pharmaceutical compositions containing the compound of formula (I): wherein D, Y, A, B, p, q, W and R have the same meanings as defined in the specification.
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Page/Page column 5
(2010/02/11)
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- Benzimidazolone antiviral agents
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The present invention concerns antiviral compounds, their compositions, and use in the treatment of viral infections. More particularly, the invention provides benzimidazolone derivatives for the treatment of respiratory syncytial virus infection.
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- Synthesis and evaluation of 2-tosylamino and 2-tosyliminopyrimidine derivatives as inhibitors of some leukocyte functions
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We have studied the potential anti-inflammatory effects of 20 2-tosylamino and 2-tosyliminopyrimidine new derivatives in human neutrophils. We have evaluated their interference with some leukocyte functions and 5-lipoxygenase activity. All the compounds r
- Fernandez-Ferri, Patricia,Ubeda, Amalia,Guillen, Isabel,Lasri, Jamal,Gonzalez-Rosende, M. Eugenia,Akssira, Mohamed,Sepulveda-Arques, Jose
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p. 289 - 296
(2007/10/03)
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- 5-SUBSTITUTED 1,1-DIOXO-`1,2,5!THIAZOLIDINE-3-ONE DERIVATIVES AS PTPASE 1B INHIBITORS
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Compounds of the formula (I) provide pharmacological agents which are inhibitors of PTPases, in particular, the compounds of formula (I) inhibit PTP-1 B and TC PTP, and thus may be employed for the treatment of conditions associated with PTPase activity.
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Page/Page column 61
(2010/02/07)
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- Laser flash photolysis studies on the first superoxide thermal source. First direct measurements of the rates of solvent-assisted 1,2-hydrogen atom shifts and a proposed new mechanism for this unusual rearrangement
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The thermal decomposition of bis(4-carboxybenzyl)hyponitrite (SOTS-1) in aerated water under physiological conditions has previously been shown to give the superoxide radical anion in a yield of 40 mol % (Ingold, K. U.; et al. J. Am. Chem. Soc. 1997, 119, 12364). The absolute kinetics of the elementary reactions involved in the cascade of events leading from the first-formed water-soluble benzyloxyl radical to superoxide have been determined by laser flash photolysis. On the basis of these kinetics it is concluded that SOTS-1 will be suitable for studies of superoxide-induced oxidative stress in most biological systems. A water-assisted 1,2-H shift converting benzyloxyl into the benzyl ketyl radical is an important step in the above reaction cascade. The kinetics of the 1,2-H shift assisted by H2O, D2O, and a number of nucleophilic alcohols have been measured for the first time. These data have led to a proposed new mechanism involving the initial formation of a ketyl radical anion and an oxonium cation which generally collapse to give the neutral ketyl radical as the first observable product on the time scale of our experiments (ca. 80 ns).
- Konya, Klara G.,Paul, Thomas,Lin, Shuqiong,Lusztyk, Janusz,Ingold
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p. 7518 - 7527
(2007/10/03)
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- Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase
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The examination results of a novel series of potential inhibitors of glycinamide ribonucleotide transformylase (GAR Tfase) and aminoimidazole carboxamide transformylase (AICAR Tfase) are reported. These agents incorporate an electrophilic fluoronitropheny
- Boger, Dale L.,Marsilje, Thomas H.,Castro, Rene A.,Hedrick, Michael P.,Jin, Qing,Baker, Stephen J.,Shim, Jae Hoon,Benkovic, Stephen J.
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p. 1471 - 1475
(2007/10/03)
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- Preparation of α-Branched Phenylalanines and of 1,1-Disubstituted Ethylenediamines via Chiral Imidazolidinones and Oxazolidinones of Glycine - Preparative and Mechanistic Aspects
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To test the structural prerequisites for a new carbanionoid rearrangement of 3-methyl-2-pivaloyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid to N-(t-butoxycarbonyl)-1-amino-2-methylindan-2-carboxylic acid (A -> B), various α-branched phenylalanines (
- Seebach, Dieter,Gees, Thomas,Schuler, Franz
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p. 785 - 800
(2007/10/02)
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- CARBOXAMIDE AMINO ACID HETEROBICYCLIC PAF ANTAGONISTS
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Compounds of general formula I; STR1 wherein R 1, R. sup.2, R. sup.3, R 4, R 5, R 6, R 7, R 8, A 1, A. sup.2, B, and X are variables.These compounds are antagonists of platelet activating factor (PAF) and as such are useful in the treatment or ameli
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- Penem derivatives
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Compounds of formula STR1 wherein R is hydrogen atom or C1 -C4 alkyl group optionally substituted from halogen atom or hydroxy group optionally protected, A is a Z, Z--O--C--O-- or Z--C)-- residue, wherein Z is phenylene, naphthylene
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- The easy preparation of many benzylic bromides using molecular bromine as a halogenating in the presence of catalytic amounts of lanthanum tri-acetate
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Many benzylic brominations were easily achieved by molecular bromine in CCl4 in presence of 1 percent of La (OAc)3 and a standard room lighting lamp.The selectivity is excellent except for certain electron-rich systems (p-methylaniline, p-cresol).
- Ouertani, Mohsen,Girard, Pierre,Kagan, Henry B.
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p. 327 - 328
(2007/10/02)
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- New, Easily Removable Poly(ethylene glycol) Supports for the Liquid-Phase Method of Peptide Synthesis
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Poly(ethylene glycol) (PEG) was derivatized with a number of acid-cleavable and photocleavable anchoring groups in order to test the applicability of these derivatives as supports in liquid-phase peptide synthesis.PEG was subjected to rapid and quantitati
- Pillai, V. N. Rajasekharan,Mutter, Manfred,Bayer, Ernst,Gatfield, Ian
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p. 5364 - 5370
(2007/10/02)
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- Haloalkylbenzoyl esters of di-lower alkylamino alkanols and quaternary lower alkyl salts thereof
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There are provided certain novel halo lower alkyl benzoyl esters of di(lower alkyl amino) lower alkanols and the quaternary salts thereof, in particular the bromomethyl benzoyl esters of dimethyl aminoethanol and choline which possess activity as insecticides and cholinesterase inhibitors. The corresponding formyl benzoyl esters exhibit similar activity.
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