P-(TRANS-4-AMINOMETHYLCYCLOHEXYLCARBONYL) PHENYLPROPIONIC ACID

摘要

PURPOSE:To extremely reduce by-products caused by self condensation and to obtain the titled compound having antitumor action industrially and in high yield, by condensing trans-4-cyanocyclohexanecarboxylic acid chloride with phenylpropionic acid ester. CONSTITUTION:A compound shown by formula I is reacted with a phenylpropionic ester shown by formula II (R is lower alkyl) in the presence of a condensation agent (e.g. aluminum chloride, ferric chloride or stannic chloride) to give a p-(trans-4-cyclohexylcarbonyl)phenylpropionic ester shown by formula III. Then this alkyl ester is hydrolyzed and then the nitrile group is reduced or the nitrile group is reduced and then the ester hydrolyzed or simultaneously the ester is hydrolyzed to give a compound shown by formula IV.