VERFAHREN ZUR HERSTELLUNG VON CEPHALOSPORINESTERN.

摘要

Cephalosporin esters of the formula I wherein R2 is hydrogen or acyl and R1 is a group which is readily removable by hydrolysis, and pharmaceutically acceptable acid addition salts of basic compounds of formula I in which R2 is an acyl group, may be prepared by reacting 7-amino-3-methyl-3-cephem-4-carboxylic acid (7-ADCA) in a partially chlorinated lower alkane with a bicyclic amidine of the formula II wherein n is the integer 3, 4 or 5, and a halide of the formula X-R1 III wherein X is halogen and R1 has the above significance, if desired, treating the resulting compound of formula I in which R2 is hydrogen with an unprotected or optionally protected acylating agent, cleaving off a protecting group which may be present and, if desired, treating a resulting basic compound of formula I in which R2 is an acyl group into a pharmaceutically acceptable acid addition salt.