| 摘要 |
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 0.4-0.1 equivalent (based on imino acid) of a base (e.g. N-methylpiperidine, triethylamine, etc.) at 0-80 deg.c. USE:Pharmaceuticals (hypotensor, etc.), agricultural chemicals and their intermediates. |
