专利号:US-4171439-A 优先权日:1975-04-11 标 题 :Antibacterial analogs of isocephalosporins 发明人:CONWAY TERRY T; LIM GARY M F; MENARD MARCEL 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 Z is halo or hydroxyl and X is acylamino. 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-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-4112230-A 优先权日:1975-04-11 标题 :Δ2,3 -1,4 Morpholine-2-carboxylic acid derivatives as antibacterial agents 发明人:MENARD MARCEL; LIM GARY M F; CONWAY TERRY T 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 Z is halo, hydroxyl, etherified hydroxyl or hydroxyl esterified with a carboxylic acid residue or a sulfonic acid residue and X is amino, azido or acylamino. 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-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-4166906-A 优先权日:1975-04-11 标题:0-2-Isocephem-4-carboxylic acid derivatives as antibacterial agents 发明人:CONWAY TERRY T; LIM GARY M F; MENARD MARCEL 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 Z is hydroxyl esterified with a sulfonic acid residue and X is acylamino. Also included in the invention are compounds of the above formula in which the carboxyl group of 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-4269773-A 优先权日:1976-04-27 标 题:Fused oxazolidine compounds 发明人:MITSURU YOSHIOKA; TERUJI TSUJI; YASUHIRO NISHITANI; WATARU NAGATA 权利人:SHIONOGI & CO 摘要:Compounds represented by the following formula prepared from 6-aminopenicillanic acid are key intermediates in a stereo-specific synthesis of 1-oxadethiacephalosporins, highly active antibiotics: +TR [wherein COA and COB each is carboxy or protected carboxy; COX is carboxy, protected carboxy, or a group of the formula -COCQ=N2 or -COCHQ-Z (in which Q is hydrogen, lower alkyl or aryl; and Z is hydrogen or a nucleophilic group); Hal is halogen; R is lower alkyl or aralkyl; and Y is hydrogen or acyl].