PURPOSE: To prepare a β-lactam antibacterial agent continuously, in high efficiency, by reacting an ester having a specific structural formula with an aminoazetidinonecarboxylic acid having a specific structural formula in an aqueous solution in the presence of an acylating enzyme.
CONSTITUTION: A β-lactam antibacterial agent which is an amide compound of formula III [RCO is acyl; Q is group of formula IV or V (Z is H, halogen, nucleophilic group, methyl, halomethyl, or nucleophilic group-substituted methyl)] is prepared by reacting an ester of formula I (X is H, lower alkyl or hydroxy-lower-alkyl; Y is H or lower alkyl; n is a positive integer) with an aminoazetidinonecarboxylic acid of formula II in the presence of an acylating enzyme in an aqueous solution. An acylating enzyme originated from bacteria or fungi is especially important for this purpose.
MITSUKI TAKASHI
FUJIWARA TAMIO
MUNEYUKI TATSUNOSUKE
