专利号:US-5215997-A 优先权日:1985-09-11 标题:Synthesis of beta-lactam compounds 发明人:HUNGERBUEHLER ERNST; KALVODA JAROSLAV 权利人:CIBA GEIGY CORP 摘要:The invention relates to an improved process for the preparation of compounds of formula ##STR1## or salts thereof, starting from compounds of formulae ##STR2## via compounds of formulae ##STR3## in which compounds R 1 is hydrogen or lower alkyl, R 2 is an organic radical which may carry a functional group which may be protected by a customary protective group R 2 o , R 3 is hydrogen or a customary carboxyl protective group R 3 o , W is a group which can be replaced by a thiocarboxylic acid radical of formula III, and Z is oxygen or sulfur.
专利号:US-4347183-A 优先权日:1981-02-02 标 题 :Process for the synthesis of penems and carbapenems 发明人:AFONSO ADRIANO; HON FRANK 权利人:SCHERING CORP 摘要:Described is a novel process for the preparation of penems and carbapenems useful as antibacterial agents which comprises the reaction of an appropriate 4-substituted-azetidine-2-one with an acid halide in the presence of a tertiary amine and an alkaline earth metal carbonate, followed by reaction of the thereby formed 1-imido-4-substituted-azetidine-2-one with a trialkyl phosphite. n Also described are novel penems useful as antibacterials which are prepared by the described process.
专利号:WO-2012062035-A1 优先权日:2010-11-12 标 题:Synthesis method for meropenem 发明人:ZHANG GONG 权利人:SHANGHAI BUDDY BIO PHARM INTERMEDIATES LTD; ZHANG GONG 摘要:Disclosed is a synthesis method for meropenem, the reaction chain whereof is represented below: [Formula IV] → [Formula V] → [Formula II] [Formula VI] → [Formula III] – Wittig → [Formula VII] → [Formula VIII] → [Formula I] Steps in the reaction are as follow: 1) the compound of Formula (IV) and the compound of Formula (V) are dissolved in an organic solvent, then, in the presence of a condensing agent, undergo a condensation reaction to obtain the compound of Formula (II); 2) the compound of Formula (II) and the compound of Formula (VI) react in the presence of a base and produce the compound of Formula (III); 3) the compound of Formula (III) is dissolved in cyclohexane, heptane, octane, toluene or xylene, then, in the presence of an organic phosphorous reagent, undergoes a Wittig ring closure reaction to obtain the compound of Formula (VII); 4) the compound of Formula (VII) is hydrolized in the presence of an acid to obtain the compound of Formula (VIII); 5) the compound of Formula (VIII) is hydrogenated in the presence of a palladium catalyst to remove allyl and obtain meropenem.
专利号:US-5191077-A 优先权日:1987-05-11 标题:Diastereomeric 5R,6S-6-(1R-hydroxyethyl)-2-(cis-1-oxo-3-thiolanylthio)-2-penem-3-carboxylic acids 发明人:VOLKMANN ROBERT A 权利人:PFIZER 摘要:Diastereomeric 5R,6S-6-(1R-hydroxyethyl)-2-(1S-oxo-3R-thiolanylthio)-2-penem-3-carboxylic acid and 5R,6S-6-(1R-hydroxyethyl)-2-(1R-oxo-3S-thiolanylthio)-2-penem-3-carboxylic acid, and pharmaceutically-acceptable salts and in vivo hydrolyzable esters thereof, useful as systemic antibacterial agents; and intermediates and processes which are useful in the said synthesis of said diastereoisomers.
专利号:US-5319103-A 优先权日:1987-05-11 标 题:Intermediate diastereomeric 5R,6S-6-(1R-hydroxyethyl)-2-(cis-1-oxo-3-thiolanylthio)-2-penem-carboxylic acids 发明人:VOLKMANN ROBERT A 权利人:PFIZER 摘要:Diastereomeric 5R,6S-6-(1R-hydroxyethyl)-2-(1S-oxo-3R-thiolanylthio)-2-penem-3-carboxylic acid and 5R,6S-6-(1R-hydroxyethyl)-2-(1R-oxo-3S-thiolanylthio)-2-penem-3-carboxylic acid, and pharmaceutically-acceptable salts and in vivo hydrolyzable esters thereof, useful as systemic antibacterial agents; and intermediates and processes which are useful in the said synthesis of said diastereoisomers.
专利号:US-5183887-A 优先权日:1989-02-02 标 题:Spirocyclic 6-amido-carbapenems and azetidinones 发明人:GREENLEE MARK L; SALZMANN THOMAS N; DININNO FRANK P 权利人:MERCK & CO INC 摘要:New antibacterial spirocyclic 6-amido carbapenems of the structural formulas: wherein R1 is hydrogen, C1-8 substituted or unsubstituted alkyl, or C6-10 substituted or unsubstituted aryl; R5 is hydrogen or a protecting group for alcohol; R6 is hydrogen or a protecting group for amido nitrogen; R7 is hydrogen or a protecting group for amido nitrogen; and R8 is hydroxy, hydrogen, C1-8 substituted or unsubstituted thioalkyl, C6-10 substituted or unsubstituted thioaryl, 5 or 6 membered, substituted or unsubstituted thioheteroaryl; and a process for their synthesis through novel spirocyclic 4-amido azetidinones are disclosed.