| 摘要 |
NEW MATERIAL:A penicillin derivative of formula I (n is 0,1 or 2), salt and ester hydrolyzable in the living body. EXAMPLE:Benzhydryl 2beta-azidomethyl-2alpha-methylpenam-3alpha-carboxylate. USE:Inhibitors against beta-lactamases. PROCESS:A penicillanic acid derivative of formula II (X is chlorine or bromine; R is a protecting group of the carboxyl group in the penicillin), e.g. benzhydryl 2beta-chloromethyl-2alpha-methylpenam-3alpha-carboxylate, is reacted with a metallic azide, e.g. sodium azide, in an amount of preferably 1-10 times of the molar equivalent of the penicillanic acid derivative of formula II in a solvent, e.g. dimethylformamide, usually at 0-60 deg.C. The reaction mixture is if necessary subjected to the oxidation, ester elimination, ester interchange and salt forming reactions to give the aimed compound of formula I . |
