FLUOROMETHYLTHIOXACEPHALOSPORIN

摘要

NEW MATERIAL:The 7beta-(fluorinated methylthioacetamido)-7alpha-methoxy-3-(nucleophilic group-substituted)methy-1-dethia-1-oxa-3-cephem-4-carboxylic acid of formula I (A is CH2F- or CHF2-; Z is nucleophilic group) and its derivative at COOH group. EXAMPLE:7beta-Difluoromethylthioacetamido-7alpha-methoxy-3-chloromethy l-1-dethia-1- oxa-3-cephem-4-carboxylic acid diphenylmethyl ester. USE:An antibacterial agent having high stability and low side effect, and effective to the bacteria resistant to other antibacterial agents. PREPARATION:The compound of formula I can be prepared e.g. by reacting the amine of formula II (B is COOH-protecting group) or its reactive derivative with the carboxylic acid of formula III or its reactive derivative preferably at -20- +50 deg.C for 10min-5hr.