Amoxycillin and analogues - from 6-APA with protected alpha-azido-hydroxy-phenylacetic anhydrides and chlorocarbonyloxy-NN-dimethyl-forminium chlorides

摘要

Prepn. of penicillins of formula (I): (where X is H or Cl; - 6-APA is the 6-aminopenicillanic acid residue) by firstly reacting 6-APA or one of its salts with bases, with a cpd. of formula (II): (where R is alkyl, benzyl or phenyl; and X is H or Cl) and reducing the prod. with H2. Amoxycillin and analogues are obtd. in high purity. The inter. (II) with an alpha-azido gp. avoids the need for protecting an alpha-amino gp.