METHOD OF (6R,7R)-(LZ)-2-(2-AMINOTHIAZOLE-4-YL)-2-(OXYIMINO)ACETAMIDO)-3-CEPHAEME-4-CARBOXYL ACID'S DERIVATIVES PREPARATION

摘要

PURPOSE:To produce the titled compound useful as an antibacterial agent, by a novel process, by condensing a novel substituted hydroxyiminoacetic acid compound with an amino cephem carboxylic acid compound. CONSTITUTION:The objective compound of formula IV can be prepared by condensing (Z)-2-aminothiazolyl-2-substituted-hydroxyiminoacetic acid compound of formula I (R<1> is H or lower alkyl; n is 2 or 3) or its reactive derivative with (6R, 7R)-7-amino-3-cephem-4-carboxylic acid compound (salt) of formula II [when R<2> is acetoxy, etc., R<4> is (protected) carboxy, and when R<2> is group of formula III (Y is H or hydroxymethyl), R<4> is -COO<->], and when R<4> is protected carboxyl, removing the protecting group. The starting compound of formula I is novel, and can be produced e.g. by reacting the butyric acid derivative of formula V (R<6> is H, etc.; X is halogen) with thiourea.