酵素的脱ベンジル化反応による4'-(2-Carboxyethyl)phenyl trans-4-Aminomethyl Cyclohexane Carboxylate Hydrochloride(Cetraxate Hydrochloride)の合成

抄録

Cetraxate hydrochloride (1) (antiulcer agent) has been industrially produced by the chemical deprotective method of p-hydroxy propionic acid derivatives. Screening of enzymes which quantitatively hydrolyzed cetraxate benzyl ester hydrochloride (2) into 1 was undertaken to establish a novel enzymatic method of production of 1. It was found that the enzyme activity for debenzylation of 2 is contained in cellulase enzymes originated from Aspergillus sp. Lower alkyl groups or phenyl groups of p-hydroxy propionic acid derivatives are likewise selectively hydrolyzed by the cellulase enzyme. This enzymatic synthetic method is very useful for the industrial preparation of 1.