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http://dx.doi.org/10.14478/ace.2022.1060

A Study on The Synthesis of Camostat Mesylate Using Vilsmeier-Haack Reaction  

Kim, Dong Nyeon (Department of Applied Chemistry, Kookmin University)
Kim, Seok Chan (Department of Applied Chemistry, Kookmin University)
Publication Information
Applied Chemistry for Engineering / v.33, no.4, 2022 , pp. 440-443 More about this Journal
Abstract
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.
Keywords
Chronic Pancreatitis; Camostat mesylate; Esterification; Vilsmeier-Haack reaction; Activating reagent;
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