专利号:US-8921580-B2 优先权日:2012-05-09 标 题 :Methods and systems for the formation of cyclic carbonates 发明人:HATTON TREVOR ALAN; JAMISON TIMOTHY F; KOZAK JENNIFER AIDEN; SIMEON FRITZ; WU JIE 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Described herein are inventive methods for synthesis of cyclic carbonates from CO 2 and epoxide. In some embodiments, the methods are carried out in the presence of a catalyst comprising an electrophilic halogen. In some embodiments, the methods are carried out in a flow reactor.
专利号:US-7220870-B2 优先权日:1995-03-14 标 题:Hydrolytic kinetic resolution of cyclic substrates 发明人:JACOBSEN ERIC N; TOKUNAGA MAKOTO; LARROW JAY F 权利人:HARVARD COLLEGE 摘要:The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.
专利号:US-5977409-A 优先权日:1997-04-15 标题 :Method of using α-substituted benzylamine chiral auxiliary synthetic reagents 发明人:ERHARDT PAUL W 权利人:UNIV TOLEDO 摘要:This invention relates to the use of a family of chiral alpha -substituted benzylamine reagents during chemical synthesis. Specifically, the reagents can be used in an auxiliary manner to deliver either a substituted or unsubstituted nitrogen atom while simultaneously bestowing an asymmetric bias toward the formation and separation of the diastereomeric intermediates that result from reaction of the reagents with racemic substrates also having one or more asymmetric atoms. The chiral auxiliary portion of the reagents can then be readily removed at some later and convenient stage of the overall synthetic scheme. The initial nitrogen-delivery reaction, asymmetric separation procedures, and removal of the chiral auxiliary can all be conducted under routine experimental conditions, including the final debenzylation, such that the overall method is adaptable to large-scale chemistry. Since the reagents are particularly useful whenever a nitrogen-containing system has alpha- , beta- or gamma-asymmetry, the latter being a common structural motif within many pharmaceutical agents, the methods are of primary utility for the laboratory preparation and large-scale manufacture of enantimerically pure drug molecules.
专利号:US-6639087-B2 优先权日:2001-08-22 标题:Kinetic resolution method 发明人:LARROW JAY F; JASMIN SERGE; LIU YI; DI MARE MARCELLO 权利人:RHODIA PHARMA SOLUTIONS INC 摘要:A method for stereoselective chemical synthesis, includes the steps of: (A) reacting a nucleophile and chiral or prochiral cyclic subtrate, said substrate comprising a carbocycle or a heterocycle having a reactive center susceptible to nucleophilic attack by the nucleophile, in the presence of a chiral non-racemic catalyst to produce a product mixture comprising a stereomerically enriched product wherein the product mixture further comprises a catalyst residue, at least a portion of the catalyst residue is in a first oxidation state, and the catalyst residue in the first oxidation state is active in catalyzing degradation of the stereoisomerically enriched product, and (B) chemically or electochemically changing the oxidation state of the catalyst residue from the first oxidation state to a second oxidation state, wherein catalyst residue in the second oxidation state is less active in catalyzing degradation of the stereoisomerically enriched product than is catalyst residue in the first oxidation state. The method reduces erosion of the chiral purity of the stereoisomerically enriched product and reduces the chemical transformation to side products of the stereoisomerically enriched product and co-product(s). The deactivated catalyst is recoverable and recyclable.
专利号:US-5153209-A 优先权日:1989-09-22 标题 :Pyridone nitriles useful in treating cardiovascular disease 发明人:WHEELER THOMAS N; KENAKIN TERRENCE P; SHAFFER JOEL E 权利人:GLAXO INC 摘要:Pyridones of formula (I) for treating congestive heart failure: ##STR1## wherein: R 1 and R 2 are a variety of phenyl substituents, L is a divalent alkylene linking group. Pharmaceutical composition, methods for their use in treating cardiovascular conditions, processes used in synthesis and intermediates used in such processes.
专利号:US-5051431-A 优先权日:1989-09-22 标题 :Pyridone nitriles useful in treating cardiovascular disease 发明人:WHEELER THOMAS N; KENAKIN TERRENCE P; SHAFFER JOEL E 权利人:GLAXO INC 摘要:Pyridones of formula (I) for treating congestive heart failure: ##STR1## wherein: R 1 and R 2 are a variety of phenyl substituents, L is a divalent alkylene or amide containing alkylene linking group. Pharmaceutical composition, methods for their use in treating cardiovascular conditions, processes used in synthesis and intermediates used in such processes.
摘要:Ogawa, C.; Kobayashi, S., Science of Synthesis: Water in Organic Synthesis, (2012) 1, 581. 摘要:Majerić Elenkov, M.; Szymański, W.; Janssen, D. B., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 2, 519. 摘要:Li, A. T.; Li, Z., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 2, 489.