专利号:US-9475814-B2 优先权日:2011-10-03 标题:Chiral N-acyl-5,6,7(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof 发明人:HOVEYDA HAMID R; DUTHEUIL GUILLAUME; FRASER GRAEME L; ROY MARIE-ODILE; EL BOUSMAQUI MOHAMED; BATT FREDERIC 权利人:EUROSCREEN SA 摘要:The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I.
专利号:US-7943769-B2 优先权日:2006-12-12 标题 :Fluorinated derivative of quinolin-2(1H)-one, method for preparing the same and use thereof as a synthesis intermediate 发明人:LEGROUX DIDIER; MORAGUES VERONIQUE; RUIZ-MONTES JOSE; SALLE LAURENT 权利人:SANOFI AVENTIS 摘要:The invention relates to a fluorinated derivate of quinolin-2(1H)-one (I), to a method for preparing the same, and to the use thereof as an intermediate in the synthesis of 7-fluoro-2-oxo-4-[2-[4-[thieno[3,2-c]pyridine-4-yl)piperazin-1-yl]ethyl]-1,2-dihydro-quinolin-1-acetamide. The invention also relates to the pharmaceutically acceptable salts thereof.
专利号:WO-2006135544-A1 优先权日:2005-06-10 标 题 :SYNTHESIS OF 11-(4[-(2-HYDROXYETHOXY)ETHYL]-PIPERAZINYL)-DIBENZO[b,f][1,4]THIAZEPINE AND ITS FUMARATE SALT 发明人:BUENGER GREG STEVEN; ALEXANDER ANATOLY 权利人:CAMBREX CHARLES CITY INC; BUENGER GREG STEVEN; ALEXANDER ANATOLY 摘要:The invention is directed a method for synthesizing l l-(4-[2-(2- hydroxyethoxy)ethyl]-piperazinyl)-dibenzo[b,f] [l,4]thiazepine (quetiapine) and for recovering quetiapine as its fumarate salt in which dibenzo[b,f][l,4]thiazepine- l l(10H)one is chlorinated in the presence of a trialkyl amine base using a slight molar excess of phosphorous oxychloride to produce l l-chloro-dibenzo[b,f] [l,4]thiazepine which then is alkylated with piperazine to l l-piperazinyldibenzo[b,f] [l,4]thiazepine, which finally is alkylated with 2-(2-chloroethoxy)ethanol.
专利号:WO-2010001407-A2 优先权日:2008-06-05 标 题:Synthesis of 11-(4-[2-(2-hydroxyethoxy)ethyl]- piperazinyl)dibenzo[b,f][1,4]thiazepine and its fumarate salt
专利号:US-5663449-A 优先权日:1989-05-19 标 题 :Intermediate compounds in the synthesis of heteroarylpiperidines, pyrrolidines and piperazines
专利号:US-2008241949-A1 优先权日:2007-03-29 标 题 :Process for preparing quetiapine fumarate 发明人:KANSAL VINOD KUMAR; AHMAD SUHAIL; LAL KANHAIYA; PATIL BHATU TUMBA 权利人:KANSAL VINOD KUMAR; AHMAD SUHAIL; LAL KANHAIYA; PATIL BHATU TUMBA 摘要:Provided is an improved synthesis of quetiapine and pharmaceutically acceptable salts.
摘要:WILLIAMS RT; 2ND ED, CHAPMAN AND HALL, 614 (1959) 摘要:Aronson, C.E. (ed.). Veterinary Pharmaceuticals & Biologicals, 1980-1981. Media, Pa.: Harwal Publishing Co., 1980., p. 19/15 摘要:Lide, DR (ed.). CRC Handbook of Chemistry and Physics. 71st ed. Boca Raton, FL: CRC Press Inc., 1990-1991., p. 3-405 摘要:Association of Official Analytical Chemists. Official Methods of Analysis. 10th ed. and supplements. Washington, DC: Association of Official Analytical Chemists, 1965. New editions through 13th ed. plus supplements, 1982., p. 13/663 38.211 摘要:Gilman, A.G., T.W. Rall, A.S. Nies and P. Taylor (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 8th ed. New York, NY. Pergamon Press, 1990., p. 966