PRODUCTION OF 2-AMINOTHIAZOLEACETIC ACID DERIVATIVE

摘要

PROBLEM TO BE SOLVED: To obtain a compound useful as an intermediate for pharmaceuticals in high yield by the alcoholytic reaction of a thiazole derivative. SOLUTION: A 2-aminothiazoleacetic acid derivative of formula II is produced by reacting a thiazole derivative of formula I (R<1> is an amino-protecting group; R<2> is an OH-protecting group; R<3> is a carboxy-protecting group) with an alcohol (e.g. methanol) at 20-80 deg.C for 1-100hr. The amount of the alcohol is 1-300 times equivalent based on the compound of formula I. An example of the compound of formula I is (Z)-2-(2-t-butoxycarbonylaminothiazol-4-yl)-2-t-acetoxyiminoacetic acid methyl ester and that of the compound of formula II is 2-(Z)-(2-t- butoxycarbonylaminothiazol-4-yl)-2-hydroxyiminoacetic acid ethyl ester.