CEPHALOSPORIN COMPOUND, ITS PRODUCTION AND INTERMEDIATE COMPOUND

摘要

PURPOSE:To obtain a new compound having excellent absorbability through digestive tracts and useful as a peroral antibacterial agent for the prevention and treatment of microbism. CONSTITUTION:The compound of formula I [R<1> is H, lower alkyl or hydroxy- protecting group; R<2> is H or lower alkyl; R<3> is COR<5> (R<5> is H, lower alkyl or lower alkenyl), CO2R<6>, SO2R<6> (R<6> is lower alkyl), CONH2, etc.; R<4> is carboxyl or esterified carboxyl] or its salt, e.g. 7-[2-(2-aminothiazol-4-yl)-2-hydroxyimino- acetamido]-3-acetylaminoxymethyl-3-cephem-4-carboxylic acid sodium salt. The compound of formula I can be produced by reacting a compound of formula II with a compound of formula III (R<7> is H or amino-protecting group) or its reactive derivative in a solvent (e.g. methylene chloride) at room temperature or under cooling. The compound has low toxicity and exhibits extremely excellent antibacterial activity against Gram-positive bacteria and Gram-negative bacteria.