专利号:US-7138526-B1 优先权日:1999-06-15 标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives 发明人:HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M 权利人:AVENTIS PHARMA INC 摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
专利号:US-9006421-B2 优先权日:2013-03-14 标题 :Cephalosporin compositions and methods of manufacture 发明人:LAI JAN-JI; PATHARE PRADIP M; KOLLA LAXMA; SORET ADRIEN F 权利人:CUBIST PHARM INC 摘要:Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising the conversion of a protected 7-amino group into a 7-carboxamide moiety in a single step.
专利号:US-4171438-A 优先权日:1975-07-23 标 题:0-2-Isocephem-4-carboxylic acid derivatives as antibacterial agents 发明人:DOUGLAS JAMES L; HORNING DONALD E; MORRIS LEESON R 权利人:BRISTOL MYERS CO 摘要:There is described the stereoselective total synthesis of novel DELTA 2,3-1,4-morpholine-2-carboxylic acids possessing a fused beta -lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula I wherein X is acylamino and Z represents optionally substituted C1-C6 alkyl, aryl or aralkyl. Also included in the invention are compounds of the above formula in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds. The compounds are potent antibacterial agents.
专利号:US-4118566-A 优先权日:1975-07-23 标 题:Δ2,3 -1,4-Morpholine-2-carboxylic acid derivatives as antibacterial agents 发明人:HORNING DONALD E; MORRIS LEESON R; DOUGLAS JAMES L 权利人:BRISTOL MYERS CO 摘要:There is described the stereoselective total synthesis of novel DELTA 2,3-1,4-morpholine-2-carboxylic acids possessing a fused beta -lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula I wherein X is amino, azido or acylamido and Z represents optionally substituted C1-C6 alkyl, aryl, aralkyl or heterocyclic. Also included in the invention are compounds of formula I in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds of formula I. The compounds of formula I are potent antibacterial agents or are of use as intermediates in the preparation of such antibacterial agents.
专利号:US-4950660-A 优先权日:1987-09-07 标 题:Beta-lactam compound and process for production thereof 发明人:ATSUMI KUNIO; YAMAMOTO YUICHI; SAKAGAMI KENJI; NISHIHATA KEN; KONDO SHINICHI 权利人:MEIJI SEIKA CO 摘要:The present invention relates to a cephem compound of formula (III) shown in the description. The compound is useful as an intermediate for the synthesis of beta -lactam antibiotics of new class and also to a process for producing the same. The cephem compound (III) is produced by reacting a cephem compound of formula (I) with a nitrogen-containing compound of formula (II) under acid-capturing conditions. The process can be performed easily under mild conditions.
专利号:US-4436912-A 优先权日:1981-09-08 标题:7-[2-(2-Aminooxazol-4-yl)-2-(oximino)acetamido cephalosporin antibiotics and intermediates therefor 发明人:WHEELER WILLIAM J 权利人:LILLY CO ELI 摘要:Cephalosporin broad spectrum antibiotics possessing a 7 beta -[2-[(2-aminooxazol)-4-yl]-2-(substituted oximino]acetamido side chain and a variety of substituents at the 3-position of the cephalosporins are claimed. Also claimed are intermediates in the synthesis of the above cephalosporin antibiotics.