PURPOSE: To obtain the titled substance preventing the decomposition and racemization, etc., of active ester group, by reacting an imino acid with a carboxylic acid thioester or an amino acid thioester in an inert organic solvent under neutral condition.
CONSTITUTION: The objective compound of formula III can be produced by reacting an imino acid of formula I (A is alkyl, hydroxyalkyl, H, alkenyl, aryl, hydroxyphenyl, etc.; B is alkyl, hydroxyalkyl, etc.; A and B may together form a ring) with a compound of formula II (R is alkyl, alkenyl, aryl, aminoalkyl, etc.) in an inert organic solvent (e.g. DMSO, DMF, etc.) in the presence of 0.4W0.1 equivalent (based on imino acid) of a base (e.g. N-methylpiperidine, triethylamine, etc.) at 0W80°c.
USE: Pharmaceuticals (hypotensor, etc.), agricultural chemicals and their intermediates.
KUROKAWA NATSUKO
HORI KEIKO
