PURPOSE: To obtain the titled compound useful as a remedy for pancreatitis industrially and advantageously in high purity, by reacting guanidinocaproic acid with ethyl p-hydroxybenzoate in the presence of a tertiary amine and a specific compound.
CONSTITUTION: Guanidinocaproic acid or an acid addition salt thereof is reacted with ethyl p-hydroxybenzoate to give p-ethoxycarbonylphenyl guanidinocaproate ester. In the process, a tertiary amine, e.g. pyridine or quinoline, and an N,N- bis(2-oxo-3-oxazolidinyl)phosphorodiamidic halide are used to afford the aimed compound and an acid addition salt thereof. Hydrochloride, sulfate, hydrobromide, etc. may be cited as the acid addition salt of the guanidinocaproic acid. The reaction process can be carried out by easy operation and is advantageous.
ADACHI TSUTOMU
TAKAHASHI MINOICHI
TAKAHASHI YOSHIO
