PURPOSE: To obtain the titled compound useful as a remedy for acute pancreatitis, etc., by reacting an anhydride of mixed acids of -ganidinocaproic acid and a lower alkyl carbonic acid with p-hydroxybenzoic acid ethyl ester in the presence of an acid-acceptor.

CONSTITUTION: -Guanidinocaproic acid shown by the formula II is reacted with a chloroformic acid alkyl ester shown by the formula III in an inert solvent (e.g., dimethylformamide) in the presence of an acid-acceptor (e.g., TEA) to give an anhydride of mixed acids shown by the formula IV, which is reacted with p-hydroxybenzoic acid ethyl ester shown by the formula V to give a compound shown by the formula I. The compound shown by the formula I has an inhibitory action on hydrolysis of tosyl-L-arginine methyl ester of kallikrein, especially its methanesulfonate is useful as a remedy for acute pancreatitis as an anti-kallikrein agent and the aimed compound is obtained inexpensively and in high yield by this method.