7-AMINO-3-SUBSTITUTED METHYL-DELTA 3-CEPHEM-4-CARBOXYLIC ACID AS INTERMEDIATE PRODUCTS IN SYNTHESIS 7-ACYLAMIDO-CEPHALOSPORINS SHOWING ANTIBACTERIAL PROPERTIES

摘要

PURPOSE:To obtain the titled compound useful as an intermediate for an antibacterial agent in high purity in high yield easily, by reacting a specific cephalosporanic acid with a triazole or tetrazole in an organic solvent in the presence of an acid or a complex of an acid. CONSTITUTION:A compound shown by the formulaI[R<1> is H or alkoxy; R<2> is NH2, or a group shown by the formula II or III (R<3>-R<7> are organic residue not participating in a reaction); X is optionally substituted acyloxy or carbamoyloxy; Y is S, or S O], derivative at its COOH, or its salt, is reacted with a triazole or tetrazole wherein C in the ring may be substituted, to give a compound shown by the formula IV, its derivative, or its salt. The reaction is carried out in an organic solvent, e.g., nitromethane, etc. in the presence of an acid or a complex of acid (e.g., sulfuric acid, BF3 or its complex compound etc.).