发明名称 CEPHALOSPORIN DERIVATIVES
摘要 NEW MATERIAL:A compound expressed by formula I [R1 is COOH or COOM (M is an alkali metal, etc.), etc.; R2 is formula II or -SR3 (R3 is a 5- or 6- membered ring, having 1-4 hetero-atoms, and optionally substituted by a lower alkyl group); n is 1 or 2] and a salt thereof. EXAMPLE:The syn-isomer of 7beta-{2-( 2- aminothiazol -4- yl )-2-[(imidazol-4-yl)methoxyimino]acetamido}-3-(1-pyridinium)methyl-3-c ephem-4-carboxylate. USE:An antimicrobial agent. PROCESS:A compound expressed by formula III (X is halogen; R4 is a protecting group of the carboxylic acid) is acylated with a compound expressed by formula IV(R5 and R6 are H, formyl, etc.) to give a compound expressed by formula V, which is then reacted with pyridine or a compound expressed by the formula HS-R3 to afford an intermediate sulfoxide expressed by formula VI. The resultant intermediate sulfoxide expressed by formula VI is then converted into a sulfide derivative. The protecting groups are then removed to afford the compound expressed by formula I .
申请公布号 ZA8301887(B) 申请公布日期 1983.11.30
申请号 ZA19830001887 申请日期 1983.03.17
申请人 DAIICHI SEIYAKU CO 发明人 MASAHIRO ARIMOTO;HIROAKI TAGAWA;MINORU FURUKAWA
分类号 C07D501/36;A61K31/545;A61K31/546;A61P31/04;C07D;C07D501/46 主分类号 C07D501/36
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