• Applied Chemistry for Engineering
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• v.33 no.4
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• pp.440-443
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• 2022

A key step in the synthesis of camostat mesylate, which is most widely used as a treatment for chronic pancreatitis, was conducted. Camostat mesylate was synthesized through the esterification reaction of two intermediates, GBA (4-guanidinobenzoic acid hydrochloride) and DOHA [2-(dimethylamino)-2-oxoethyl-2-(4-hydroxyphenyl)acetate]. In order to overcome the problem raised due to the low yield and expensive reagents, a new economical synthesis method was developed that can produce camostat mesylate with a high yield of 80% by activating the acid functional group of GBA using the Vilsmeier-Haack reaction and coupling it with DOHA.