Preparation and properties of 7α-formamido cephalosporins

Abstract

The preparation of novel antibacterially active 7α-formamido cephalosporins from the corresponding 7α-(methylthio) analogues by mercury (II)-mediated displacement with ammonia and subsequent formylation is described. The amine (2), a versatile intermediate, was prepared and acylated to give a wider range of 7α-formamido cephalosporins. Modifications at C-3 are discussed, in particular the preparation of the 3-(heterocyclylthiomethyl) cephalosporin (44) and the 3-(pyridylmethyl) derivative (49).