专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
专利号:US-8278440-B2 优先权日:2010-02-17 标 题:Process for the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:PEGLION JEAN-LOUIS; CAIGNARD PASCAL 权利人:PEGLION JEAN-LOUIS; CAIGNARD PASCAL; SERVIER LAB 摘要:Process for the synthesis of ivabradine of formula (I): n nand addition salts thereof with a pharmaceutically acceptable acid.
专利号:US-5300638-A 优先权日:1991-07-31 标题:Asymmetric synthesis of taxol side chain 发明人:FARINA VITTORIO; HAUCK SHEILA I 权利人:BRISTOL MYERS SQUIBB CO 摘要:The present invention relates to a process for the preparation of (3R, 4S)-3-hydroxy-4-phenyl-2-azetidinone derivatives which are useful intermediates in the synthesis of taxol from baccatin III, said process comprises reacting an acyloxyacetyl halide with an imine derived from L-threonine; and to compounds of formula (III) which are produced in said process: ##STR1## wherein Ar is phenyl; R 1 is hydrogen, an acyl radical of a carboxylic acid, or a carbonic acid ester radical; R 2 is hydrogen or a carboxy protecting group; and R 3 is hydrogen or a hydroxy protecting group.
专利号:WO-9316981-A1 优先权日:1992-02-28 标 题:Synthesis of ioversol using a minimal excess of acetoxyacetylchloride 发明人:MC CARTHY WILLIAM Z; KNELLER MILLS THOMAS; LIN YOULIN; WALLACE REBECCA ABERNATHY; WHITE DAVID HILL 权利人:MALLINCKRODT MEDICAL INC 摘要:The use of a minimal excess of acetoxyacetylchloride as a reagent in the synthesis of N, N'-bis (2,3-dihydroxypropyl)-5-N-(2-hydroxyethyl)glycolamido-2,4,6-triiodoisophthalamide.
专利号:US-5177261-A 优先权日:1991-07-22 标题 :Synthesis of ioversol using chloroacetyl chloride 发明人:MCCARTHY WILLIAM Z; KNELLER MILLS T; LIN YOULIN; WHITE DAVID H 权利人:MALLINCKRODT MEDICAL INC 摘要:The use of chloroacetylchloride as an alternative or substitute reagent for acetoxychloride in the synthesis of N,N'- bis (2,3-dihydroxypropyl)-5-N-(2-hydroxyethyl)glycolamido-2,4,6-triiodoisophthalamide.
专利号:US-5371278-A 优先权日:1994-03-25 标题 :Synthesis of ioversol using a minimal excess of acetoxyacetylchloride 发明人:MCCARTHY WILLIAM Z; KNELLER MILLS T; LIN YOULIN; WALLACE REBECCA A; WHITE DAVID H 权利人:MALLINCKRODT MEDICAL PMC 摘要:The use of a minimal excess of acetoxyacetylchloride as a reagent in the synthesis of N,N'-bis(2,3-dihydroxypropyl)-5-N-(2-hydroxy-ethyl)glycolamido-2,4,6-triiodoisophthalamide.