专利号:US-5523411-A 优先权日:1994-03-14 标题 :Synthesis of mitomycin and its analogs 发明人:JIMENEZ LESLIE; WANG ZHENG 权利人:UNIV RUTGERS 摘要:The present invention relates to the synthesis of mitomycin and analogs thereof that are useful as anticancer antibiotics. The invention further relates to analogs of mitomycin, which can be prepared according to the methods of synthesis provided. The synthetic method of the invention provides for reacting a derivitized indole with a dialkylvinylsulfonium salt to yield a tricyclic skeleton having the precursors of the fourth ring in one step, followed by an oxidation step or steps to close the fourth ring and prepare mitomycin or a related compound.
专利号:US-4914214-A 优先权日:1987-09-17 标 题:Process for the industrial synthesis of perindopril 发明人:VINCENT MICHEL; BALIARDA JEAN; MARCHAND BERNARD; REMOND GEORGES 权利人:ADIR 摘要:Process for the industrial synthesis of perindopril, in which (2S,3aS,7aS)-2-carboxyperhydroindole is condensed with N-[(S)-1-carbethoxybutyl]-(S)-alanine after protection of the carboxyl group, the product resulting from the condensation being then subjected to deprotection of the carboxyl carried by the heterocyclic ring. n The (2S,3aS,7aS)-2-carboxyperhydroindole and N-[(S)-1-carbethoxybutyl]-(S)-alanine are themselves obtained in excellent conditions from 2-carboxyindole and from L-alanine respectively, both available on an industrial scale.
专利号:US-4954640-A 优先权日:1987-09-17 标 题:Alpha-methyl benzyl amine salt of indoline -2- carboxylic acid 发明人:VINCENT MICHEL; BALIARDA JEAN; MARCHAND BERNARD; REMOND GEORGES 权利人:ADIR 摘要:Process for the industrial synthesis of (2S, 3 7aS)-2-carboxyperhydroindole by reduction of 2-carbox indole or of one of its esters to (R,S)-2-carboxyindo or of one of its esters which, after saponification, converted into the acid, the S isomer cf (R,S)-2-carboxyindoline being obtained by precipitation from the mixture of the two (R) and (S) isomers, in the presence of (+) methylbenzylamine, (S)-2-carboxyindoline being in its turn subjected to catalytic hydrogenation to give (2S, 3aS,7aS)-2-carboxyperhydroindole, after separation of (2S,3aR,7aR) isomer by crystallization. Application to the synthesis of carboxyalkyl d peptides capable of being employed in therapeutics.
专利号:US-4727183-A 优先权日:1983-12-23 标题:Process for the asymmetric synthesis of chiral α-hydroxy-2-nitrobenzenepropanoic acid 发明人:BUZBY JR GEORGE C; WINKLEY MICHAEL W; MCCAULLY RONALD J 权利人:AMERICAN HOME PROD 摘要:Disclosed herein is a process for producing an asymmetric indoline-2-carboxylic acid of the structural Formula: ##STR1## wherein X is hydrogen, bromine, chlorine, C 1-4 alkyl or C 1-4 alkoxy, which comprises: n (a) assymetrically reducing an o-nitrophenylpyruvic acid III by contacting the acid III with a reducing complex formed from (R)-proline or (S)-proline, respectively, and sodium borohydride in an inert solvent to form, respectively, an (S) or (R)-α-hydroxy-2-nitrobenzenepropanoic acid IV; n (b) reacting, respectively, said (S) or (R)-α-hydroxy-2-nitrobenzenepropanoic acid III with a Vilsmeier chlorinating reagent in which the chlorinating agent thereof is selected from a group consisting of thionyl chloride, oxalyl chloride, phosphorus oxychloride, phosphorus pentachloride and sulfuryl chloride and the amide thereof is selected from a group consisting of dimethylformamide, diethylformamide, dimethylacetamide and diethylacetamide, said reaction being run at temperatures of at least 20° C., in order to obtain, respectively, and (R) or (S)-α-chloro-2-nitrobenzenepropanoic acid IV; n (c) reducing the nitro group of said (R) or (S)-α-chloro-2-nitrobenzenepropanoic acid (V) to an amino group; and n (d) cyclizing the resulting (R) or (S)-α-chloro-2-aminobenzenepropanoic acid in aqueous base.
专利号:US-8399502-B2 优先权日:2008-09-17 标 题 :Analogs of indole-3-carbinol and their use as agents against infection 发明人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN 权利人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN; STANFORD RES INST INT 摘要:Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane, 2′,3-diindolylmethane, and 3,3′-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.
专利号:US-4644081-A 优先权日:1985-02-11 标题:Process for the asymmetric synthesis of chiral indoline-2-carboxylic acids 发明人:BUZBY JR GEORGE C; WINKLEY MICHAEL W; MCCAULLY RONALD J 权利人:AMERICAN HOME PROD 摘要:Disclosed herein is a process for producing an asymmetric indoline-2-carboxylic acid of the structural Formula: ##STR1## wherein X is hydrogen, bromine, chlorine, C 1-4 alkyl or C 1-4 alkoxy, which comprises: n (a) assymetrically reducing an o-nitrophenylpyruvic acid III by contacting the acid III with a reducing complex formed from (R)-proline or (S)-proline, respectively, and sodium borohydride in an inert solvent to form, respectively, an (S) or (R)-α-hydroxy-2-nitrobenzenepropanoic acid IV; n (b) reacting, respectively, said (S) or (R)-α-hydroxy-2-nitrobenzenepropanoic acid III with a Vilsmeier chlorinating reagent in which the chlorinating agent thereof is selected from a group consisting of thionyl chloride, oxalyl chloride, phosphorus oxychloride, phosphorus pentachloride and sulfuryl chloride and the amide thereof is selected from a group consisting of dimethylformamide, diethylformamide, dimethylacetamide and diethylacetamide, said reaction being run at temperatures of at least 20° C., in order to obtain, respectively, and (R) or (S)-α-chloro-2-nitrobenzenepropanoic acid IV; n (c) reducing the nitro group of said (R) or (S)-α-chloro-2-nitrobenzenepropanoic acid (V) to an amino group; and n (d) cyclizing the resulting (R) or (S)-α-chloro-2-aminobenzenepropanoic acid in aqueous base.
摘要:Li, H.; Mazet, C., Science of Synthesis Knowledge Updates, (2015) 2, 39. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 326. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 270. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 87. 摘要:Joule, J. A., Science of Synthesis Knowledge Updates, (2010) 2, 244.