专利号:US-2011130567-A1 优先权日:2009-06-03 标题 :Steroselective synthesis of certain trifluoromethyl-substituted alcohols 发明人:FANDRICK DANIEL R; REEVES JONATHAN T; SONG JINHUA J; TAN ZHULIN; QU BO; YEE NATHAN K; RODRIGUEZ SONIA 权利人:BOEHRINGER INGELHEIM INT 摘要:A process for stereoselective synthesis of a compound of Formula (X) n n n n n n n n n n wherein:n R 1 is an aryl group substituted with one to three substituent groups,n wherein each substituent group of R 1 is independently C 1 -C 5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, halogen, carboxy, cyano, or trifluoromethyl,n wherein each substituent group of R 1 is optionally independently substituted with one to three substituents selected from C 1 -C 3 alkyl, C 1 -C 3 alkoxy, phenyl, and alkoxyphenyl; n n R 2 and R 3 are each independently C 1 -C 5 alkyl; R 4 is C 1 -C 5 alkyl optionally independently substituted with one to three substituent groups,n wherein each substituent group of R 4 is independently C 1 -C 3 alkyl, hydroxy, halogen, amino, or oxo; and n R 5 is a heteroaryl group substituted with one to three substituent groups,n wherein each substituent group of R 5 is independently C 1 -C 5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, alkylsulfonylamino, aminosulfonyl, C 1 -C 5 alkylaminosulfonyl, C 1 -C 5 dialkylaminosulfonyl, halogen, hydroxy, carboxy, cyano, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, or C 1 -C 5 alkylthio wherein the sulfur atom is optionally oxidized to a sulfoxide or sulfone.
专利号:US-7348436-B2 优先权日:2004-03-02 标题 :Compounds useful for the synthesis of (+)-discodermolide and methods thereof 发明人:MYLES DAVID C; SHAW SIMON JAMES; SUNDERMANN KURT F 权利人:KOSAN BIOSCIENCES INC 摘要:Compounds and methods useful for the synthesis of (+)-discodermolide, a naturally occurring microtubule stabilizing agent useful as an anti-cancer agent.
专利号:US-2011130578-A1 优先权日:2009-06-03 标题 :Stereoselective synthesis of certain trifluoromethyl-substituted alcohols 发明人:FANDRICK DANIEL R; KUZMICH DANIEL; REEVES JONATHAN T; SONG JINHUA J; TAN ZHULIN; LEE THOMAS 权利人:BOEHRINGER INGELHEIM INT 摘要:A process for stereoselective synthesis of a compound of Formula (X) or Formula (X′) n n n n n n n n n n wherein:n R 1 is an aryl group substituted with one to three substituent groups,n wherein each substituent group of R 1 is independently C 1 -C 5 alkyl, C 2 -C 5 alkenyl, C 2 -C 5 alkynyl, C 1 -C 5 alkoxy, C 1 -C 5 alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, C 1 -C 5 alkoxycarbonylamino, aminosulfonyl, C 1 -C 5 alkylaminosulfonyl, C 1 -C 5 dialkylaminosulfonyl, halogen, hydroxy, carboxy, cyano, trifluoromethyl, trifluoromethoxy, nitro, or C 1 -C 5 alkylthio wherein the sulfur atom is oxidized to sulfoxide or sulfone, and n R 2 and R 3 are each independently hydrogen or C 1 -C 5 alkyl.
专利号:WO-9746543-A1 优先权日:1996-05-31 标题:Acetyl derivatives of thiazoles and analogues 发明人:PYNE STEPHEN GEOFFREY; UNG ALISON THAVARY 权利人:UNIV WOLLONGONG; PYNE STEPHEN GEOFFREY; UNG ALISON THAVARY 摘要:The present invention is directed to compounds useful in the treatment of autoimmune diseases and inflammatory diseases of general formula (I) wherein R1 is alkyl, alkenyl or alkynyl having from 1 to 6 carbons, phenyl, benzyl or phenethyl; R2 is H, C1 to C5 alkyl which can optionally be partially hydroxylated or the group (a) wherein n is from 0 to 4; and X, Y and Z are independently CH, N, NH, O or S, or a pharmaceutically acceptable ester or acid addition salt thereof, or a stereoisomer or a geometric isomer thereof, with the proviso that at least one of X, Y or Z is CH, that one and only one of X, Y and Z is NH, O or S and further that when Y is N or NH then Z is not N or NH. The present invention is also concerned with processes for the synthesis of the compounds and with methods of use of the compounds.
专利号:US-9776966-B2 优先权日:2011-03-03 标 题:Synthesis of 2-carboxamide cycloamino urea derivatives 发明人:ERB BERNHARD; GALLOU ISABELLE SYLVIE; KLEINBECK FLORIAN KARL 权利人:NOVARTIS AG 摘要:Provided herein are processes and intermediate compounds useful for the preparation of 2-carboxamide cycloamino urea derivatives, and useful intermediates therefore.
专利号:US-7521478-B2 优先权日:2002-07-30 标 题 :Total synthesis of myriaporones 发明人:DEL POZO LOSADA CARLOS; FRANCESCH ANDRES; MARCHANTE CARMEN CUEVAS; ALVAREZ MARTA PEREZ 权利人:PHARMA MAR SAU 摘要:Compounds of the general formula (I) or a pharmaceutically acceptable salt, derivative, prodrug or stereoisomer thereof are provided: wherein the substituent groups defined by R are each independently selected from the group consisting of H, SiR′ 3 , SOR′, SO 2 X, C(â•?O)R′, C(â•?O)OR′, C(â•?O)NR′, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, aryl, heteroaryl or aralkyl; the group R′ is selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, aminoalkyl, aryl, aralkyl and heterocyclic groups; and the group R″ is selected from the group consisting of H, OH, OR′, OCOR′, SH, SR′, SOR′, SO 2 R′, NO 2 , NH 2 , NHR′, N(R′) 2 , NHCOR′, N(COR′) 2 , NHSO 2 R′, CN, halogen, C(â•?O)H, C(â•?O)R′, CO 2 H, CO 2 R′, CH 2 OR, substituted or unsubstituted alkyl, substituted or unsubstituted haloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkylidene, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; with the proviso that the compound is not compound 1, 3 or 4 of U.S. Pat.No. 5,514,708. The compounds have antitumour activity. A synthetic route is also provided.
[参考文献]: Xue Zhi Zhao, Et Al. Biotinylated Biphenyl Ketone-Containing 2,4-Dioxobutanoic Acids Designed As Hiv-1 Integrase Photoaffinity Ligands. Bioorg Med Chem. 2006 Dec 1;14(23):7816-25.
合成参考文献
摘要:Mérour, J.-Y.; Joseph, B., Science of Synthesis Knowledge Updates, (2016) 3, 59. 摘要:Irudayanathan, F. M.; Lee, S., Science of Synthesis Knowledge Updates, (2019) 2, 23. 摘要:Shi, L., Science of Synthesis: Knowledge Updates, (2024) 1, 22.