专利号:US-7420052-B2 优先权日:2001-08-24 标 题:Intermediates for synthesis of vinblastine, process for preparation of the intermediates and process for synthesis of vinblastines 发明人:FUKUYAMA TOHRU; TOKUYAMA HIDETOSHI; YOKOSHIMA SATOSHI 权利人:JAPAN SCIENCE & TECH AGENCY 摘要:An intermediate for vinblastine synthesis represented by general formula A. n ngeneral formula A.n n(in the formula, R 1 , R 2 , R 3 and R 4 are the group selected independently from the group consisting of H, lower alkyl group, lower alkoxy group, halogen, lower perfluoroalkyl group, lower alkylthio group, hydroxy group, amino group, mono- or di-alkyl or acylamino group, lower alkyl or arylsulfonyloxy group. R 5 is H, or a lower alkyl group or a substituted or non-substituted aryl group, R 6 is an alkyl group of carbon number 4 or less, R 7 is a substituted or non-substituted aryl group, R 8 is a substituted or non-substituted aryl group or lower alkyl group and R 9 is an acyl group or trialkylsilyl group.) A method for synthesis of the compound of general formula A utilizing radical ring forming reaction of thioanilides and using the compound of general formula B as the starting material, synthesizing thioanilide of general formula C by the reaction with compound 1 and the formation of a 11-membered ring by intramolecular alkylation of 2-nitrobenzenesulfonamide by which the reactions can proceed under mild conditions and high yield can be accomplished.
专利号:US-8026384-B2 优先权日:2007-05-04 标题:Process for the synthesis of alkyl phosphinic acids by initiation of an amine and an amineoxide 发明人:FINNHULT DANIEL; SOHLBERG ROGER; STALFORS FREDRIK; SVENSSON CARINA; WACHTMEISTER JOHANNA; WANNMAN THOMAS 权利人:ASTRAZENECA AB 摘要:The present invention relates to a new process for the synthesis of alkyl phosphinic acids, and more particularly to a coupling reaction between an alkylhalide and a hypophosphorous acid derivative in the presence of an amine and an amineoxide.
专利号:WO-2008136745-A1 优先权日:2007-05-04 标题:Process for the synthesis of alkyl phosphinic acids by initiation of an amine and an amineoxide 发明人:FINNHULT DANIEL; SOHLBERG ROGER; STAALFORS FREDRIK; SVENSSON CARINA; WACHTMEISTER JOHANNA; WAENNMAN THOMAS 权利人:ASTRAZENECA AB; FINNHULT DANIEL; SOHLBERG ROGER; STAALFORS FREDRIK; SVENSSON CARINA; WACHTMEISTER JOHANNA; WAENNMAN THOMAS 摘要:The present invention relates toa new process for the synthesis of alkyl phosphinic acids, and more particularly to a coupling reaction between an alkylhalide and a hypophosphorous acid derivative in the presence of an amine and an amineoxide.
专利号:US-8962858-B2 优先权日:2011-01-21 标题 :Methods and compounds useful in the synthesis of fused aminodihydrothiazine derivatives 发明人:MITASEV BRANKO; KIM DAE-SHIK; ZHANG HUIMING; FARTHING CHRISTOPHER N 权利人:EISAI R&D MAN CO LTD 摘要:Provided are compounds and methods useful for the preparation of compounds useful as inhibitors of beta-site amyloid precursor protein (APP)-cleaving enzyme.
专利号:US-5530124-A 优先权日:1994-06-30 标 题:Method for preparing cyclic ureas and their use for the synthesis of HIV protease inhibitors 发明人:RADESCA LILIAN A; HARRIS GREGORY D; WAT EDWARD K W; WALTERMIRE ROBERT E 权利人:DU PONT MERCK PHARMA 摘要:This invention provides improved synthetic processes for the preparation of hydroxy-protected cyclic urea compounds of Formula (IX), ##STR1## which are useful as intermediates for the preparation of cyclic urea human immunodeficiency virus (HIV) protease inhibitors, from N-protected aminoaldehydes. The processes of the present invention provide high yields, can be conducted on multikilogram scale, and eliminate the need for chromatographic purification of intermediates or final product.
专利号:US-7238802-B2 优先权日:2001-08-24 标题:Intermediates for synthesis of vinblastines, process for preparation of the intermediates and process for synthesis on vinblastines
摘要:Gosmini, C.; Corpet, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 683. 摘要:U.S. Army Armament Research & Development Command, Chemical Systems Laboratory, NIOSH Exchange Chemicals., NX#02089 摘要:Ying, J.; Wu, X.-F., Science of Synthesis: Knowledge Updates, (2024) 1, 291.