专利号:US-9446995-B2 优先权日:2012-05-21 标 题:Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions 发明人:CHONG HYUN-SOON 权利人:CHONG HYUN-SOON; ILLINOIS INST OF TECH 摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
专利号:US-2010173100-A1 优先权日:2006-01-16 标题 :Method for the synthesis of product molecules 发明人:WEISS HORST; GERBER GUSTAV; NUERNBERGER PATRICK HENNING; WOLPERT DANIEL STEPHAN 权利人:BASF AG 摘要:The invention relates to a method for the synthesis of product molecules, wherein ultrashort laser pulses shaped with the aid of a pulse shaper are generated and a gas which contains educt molecules is fed onto a surface, on which the educt molecules are at least partially adsorbed, the shaped ultrashort laser pulses being directed onto the surface in order to control a reaction process for synthesis of the product molecules from educts adsorbed on the surface.
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-6204337-B1 优先权日:1996-11-19 标 题:Solid-phase synthesis of codeine from morphine 发明人:CORCORAN ROBERT C; MA JUNNING 权利人:UNIV COMMUNITY COLLEGE SYS NEV 摘要:The specification describes a methylation resin comprising methyl(dialkyl)anilinium salts or methyl(diaryl)anilinium salts covalently bonded to the resin. The methylation resin is used in the solid-phase synthesis of codeine from morphine. Accordingly, the specification describes a process for methylating morphine to form codeine by loading morphine onto a methylation resin comprising methyl(dialkyl)anilinium salts or methyl(diaryl)anilinium salts covalently bonded to the resin; contacting the loaded resin with sufficient hydrocarbon or ether solvent to cover the loaded resin; and heating the loaded resin in the hydrocarbon or ether solvent under sufficient conditions to form codeine. The methylating resin may be used to methylate phenolic moieties on other compounds and to esterify compounds containing carboxylic acid moieties.
专利号:US-5981750-A 优先权日:1995-11-21 标 题 :Solid-phase synthesis of codeine from morphine 发明人:CORCORAN ROBERT C; MA JUNNING 权利人:UNIV COMMUNITY COLLEGE SYS NEV 摘要:The specification describes a methylation resin comprising methyl(dialkyl)anilinium salts or methyl(diaryl)anilinium salts covalently bonded to the resin. The methylation resin is used in the solid-phase synthesis of codeine from morphine. Accordingly, the specification describes a process for methylating morphine to form codeine by loading morphine onto a methylation resin comprising methyl(dialkyl)anilinium salts or methyl(diaryl)anilinium salts covalently bonded to the resin; contacting the loaded resin with sufficient hydrocarbon or ether solvent to cover the loaded resin; and heating the loaded resin in the hydrocarbon or ether solvent under sufficient conditions to form codeine. The methylating resin may be used to methylate phenolic moieties on other compounds and to esterify compounds containing carboxylic acid moieties.
专利号:WO-2018154596-A1 优先权日:2017-02-22 标 题 :Process for synthesis of tiotropium bromide monohydrate 发明人:REDDY G NITHUN; REDDY G SAMHITHA; REDDY G MADAALASA; RAMANI M; REDDY G PRATAP 权利人:GBR LABORATORIES PVT LTD; RACHANA PHARMA TECH 摘要:Provided herein is a process for synthesis of tiotropium bromide wherein the coupling of scopine with 2, 2-dithienyl glycolate is achieved by a two step process under mild conditions.