专利号:US-8779122-B2 优先权日:2012-11-08 标 题:Process for the synthesis of (2E)-3-(3,4-dimethoxyphenyl)prop-2-enenitrile, and application in the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:CARRANZA MARIA DEL PILAR; GARCIA ARANDA MARIA ISABEL; GONZALEZ JOSÉ LORENZO; SANCHEZ FRÉDÉRIC 权利人:SERVIER LAB 摘要:Process for the synthesis of the compound of formula (I): n nApplication in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
专利号:US-8604213-B2 优先权日:2008-10-21 标 题 :Fluorination of aromatic ring systems 发明人:DIMAGNO STEPHEN 权利人:DIMAGNO STEPHEN; NUTECH VENTURES 摘要:This disclosure relates to reagents and methods useful in the synthesis of aryl fluorides, for example, in the preparation of 18 F labeled radiotracers. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.
专利号:US-8530689-B2 优先权日:2008-05-05 标 题 :Processes for the preparation of biphenyl compounds 发明人:PERCEC VIRGIL; ROSEN BRAD MATTHEW; WILSON DANIELA A; WILSON CHRISTOPHER J 权利人:PERCEC VIRGIL; ROSEN BRAD MATTHEW; WILSON DANIELA A; WILSON CHRISTOPHER J; UNIV PENNSYLVANIA 摘要:The invention concerns processes for the synthesis of a compound of the formula: wherein: R 1 and R 2 are each, independently, C 1 -C 12 alkyl, CO 2 R 3 , OR 4 , R 5 (OR 6 ), or C 6 -C 18 aryl; R 3 -R 6 are each, independently, C 1 -C 12 alkyl or C 6 -C 12 aryl; and n and m are each, independently, O or an integer from 1-5; said process comprising:—contacting a compound of the formula H0-R 7 -0H with BH 3 and a compound of the formula in the presence of a nickel-containing catalyst to produce a first product, where R 7 is a C 2 -C 12 hydrocarbon group and X is a halogen, OMs or OTs;—contacting the first product in situ with a compound of the formula: in the presence of a nickel-containing catalyst to produce a compound of formula I, where Z is a halogen.
专利号:US-7884125-B2 优先权日:2008-04-30 标 题:Straightforward entry to 7-azabicyclo[2.2.1]heptane-1-carbonitriles and subsequent synthesis of epibatidine analogues 发明人:STEVENS CHRISTIAN; HEUGEBAERT THOMAS 权利人:UNIV GENT 摘要:The present invention relates to a group of substituted-7-azabicyclo-[2.2.1]heptyl derivatives with biological activity. The present invention also relates to synthetic methods for producing said substituted-7-azabicyclo-[2.2.1]heptyl derivatives. The present invention also relates to certain intermediates for producing such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as a synthetic method for producing such intermediates. The present invention also relates to pharmaceutical compositions comprising such substituted-7-azabicyclo-[2.2.1]heptyl derivatives, as well as their use as medicaments for the treatment of diseases mediated by a Nicotinic Acetylcholine Receptor or a receptor being a member of the Neurotransmitter-gated Ion Channel Superfamily, such as pain, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy and nicotine addiction.
专利号:US-6465693-B2 优先权日:1998-02-26 标 题 :Metal-catalyzed arylations of hydrazines, hydrazones, and related substrates 发明人:BUCHWALD STEPHEN L; WAGAW SEBLE; GEIS O 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:A method is provided for the transition metal-catalyzed arylation, or vinylation, of hydrazines, hydrazones, and the like. Additionally, the invention provides a conceptually novel strategy, the cornerstone of which is the transition metal-catalyzed arylation or vinylation method, for the synthesis of indoles, carbazoles, and the like. The methods and strategies of the invention may be utilized in standard, parallel, and combinatorial synthetic protocols.
专利号:EP-1058678-B1 优先权日:1998-02-26 标 题:Metal-catalyzed arylations and vinylations of hydrazines, hydrazones, hydroxylamines and oximes 发明人:BUCHWALD STEPHEN L; WAGAW SEBLE; GEIS OLIVER 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:A method is provided for the transition metal-catalyzed arylation, or vinylation, of hydrazines, hydrazones, and the like. Additionally, the invention provides a conceptually novel strategy, the cornerstone of which is the transition metal-catalyzed arylation or vinylation method, for the synthesis of indoles, carbazoles, and the like. The methods and strategies of the invention may be utilized in standard, parallel, and combinatorial synthetic protocols.
摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 35. 摘要:Chen, C.; Yu, L., Science of Synthesis Knowledge Updates, (2019) 3, 133. 摘要:Singh, F. V., Science of Synthesis Knowledge Updates, (2021) 1, 168. 摘要:Rudzinski, D. M.; Leadbeater, N. E., Science of Synthesis Knowledge Updates, (2012) 1, 358. 摘要:Collings, J. C., Science of Synthesis Knowledge Updates, (2013) 4, 334.