专利号:US-5654473-A 优先权日:1995-03-16 标题:Intermediates for the synthesis of trifluoromethylated organic compounds 发明人:VAN DER PUY MICHAEL 权利人:ALLIED SIGNAL INC 摘要:Novel trifluoromethylated intermediates are provided which are useful in synthesizing trifluoromethylated organic compounds. Specifically, compounds of the formula CF 3 CClâ•?CHCH 2 X are provided, which compounds are versatile intermediates for the synthesis of a wide variety of trifluoromethylated organic compounds.
专利号:US-6111130-A 优先权日:1998-05-14 标题:Process for the preparation of trifluoromethyl containing derivatives 发明人:VAN DER PUY MICHAEL 权利人:ALLIED SIGNAL INC 摘要:The present invention relates to a process for the preparation of trifluoromethylated derivatives of the formula CF 3 CClâ•?CHCH 2 OC(â•?O)R, wherein R is unsubstituted or substituted C 1 to C 6 straight chain or branched alkyl, unsubstituted or substituted C 3 to C 7 cycloalkyl, unsubstituted or substituted C 2 to C 12 alkenyl, a benzyl group unsubstituted or substituted with R', a phenyl group unsubstituted or substituted with R'; R' is an unsubstituted or substituted C 1 to C 6 straight chain or branched alkyl; and wherein where R and/or R' are substituted each is substituted with R', by reaction of HCFC-353 with carboxylic acid salts. The trifluoromethylated derivatives, particularly CF 3 CClâ•?CHCH 2 OC(â•?O)CH 3 , are versatile intermediates for the synthesis of a wide variety of trifluoromethylated organic compounds, which find utility as pharmaceuticals, agricultural chemicals, and materials such as liquid crystals.
专利号:US-2008280855-A1 优先权日:2005-06-22 标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles 发明人:CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO 权利人:NYCOMED GMBH 摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.
专利号:WO-2007141253-A1 优先权日:2006-06-07 标 题 :Process for the production of intermediates for the preparation of tricyclic imidazopyridines 发明人:PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; CHIESA MARIA VITTORIA; ZANOTTI-GEROSA ANTONIO 权利人:NYCOMED GMBH; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; CHIESA MARIA VITTORIA; ZANOTTI-GEROSA ANTONIO 摘要:The invention relates to a process for the synthesis of compounds of the formula (1-a) and compounds of the formula (1-b). The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Arom have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.
专利号:US-2006167268-A1 优先权日:2002-04-09 标 题:Growth hormone secretagogues 发明人:EVERS BRITTA; GERD RUEHTER; MARTIN DE LA NAVA EVA M; TEBBE MARK J 权利人:ELI LILLY AND COMPANY PATENT D 摘要:This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for use in the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.
专利号:US-7420070-B2 优先权日:2000-12-28 标 题:Process for preparing optically active 2,3-dihydrobenzofuran compounds 发明人:AOKI ISAO; ADACHI MARI; TAWADA HIROYUKI; YAMASHITA MAKOTO; SERA MISAYO 权利人:TAKODA PHARMACEUTICAL COMPANY 摘要:A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound: n n[wherein R 1 and R 2 are each hydrogen or an optionally substituted hydrocarbon group; R 3 is an optionally substituted aromatic group; and C is a benzene ring which may further have a substituent in addition to the amino group]. The process enables industrially advantageous production of intermediates for the synthesis of optically active 2,3-dihydrobenzofuran compounds useful as preventive and/or therapeutic drugs for neurodegenerative diseases and so on.
参考文献:10.1021/jm051091j 摘要:Frédérick R, Dumont W, Ooms F, Aschenbach L, Van der Schyf CJ, Castagnoli N, Wouters J, Krief A. Synthesis, Structural Reassignment, and Biological Activity of Type B MAO Inhibitors Based on the 5H-Indeno[1,2-c]pyridazin-5-one Core. J. Med. Chem. 2006 May 17;49(12):3743–7. doi: 10.1021/jm051091j.