To efficiently obtain 6-aminoacyl-penicillin or the like useful as an antimicrobial agent or the like in high purity and high yield by acylating silylated 6-amino-penicillanic acid or the like obtained under a specified condition.
7-Amino-desacetoxy-cephalosporanic acid or 6-amino-penicillanic acid is silylated in a carboxylic ester of the formula X-COO-Y (X is methyl; and Y is a 3-8C alkyl) to provide a silylated 7-amino-desacetoxy-cephalosporanic acid or a silylated 6-amino-penicillanic acid, and the obtained silylated compound is acylated by using a proper acylation agent to provide the objective 6- aminoacyl-penicillin or 7-aminoacyl-desacetoxy-cephalosporin except amoxicillin. Isopropyl acetate or n-butyl acetate are preferable as the carboxylic ester.
DIAGO JOSE
LUDESCHER JOHANNES
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