Chen Guohua
2013
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0
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Journal
Chinese Journal of Applied Chemistry
Abstract
4-Methylamino-3-nitrobenzoic acid(3) was prepared from 3-nitro-4-chlorobenzoic acid by methylamination.3-[(Pyridin-2-yl)amino]propinoic acid ethyl ester(5) was prepared from 2-aminopyridine and ethyl acrylate by Michael addition.Dabigatran etexilate was synthesized from compounds 3 and 5 via condensation,catalytic hydrogenation,acylation with N-(4-cyanophenyl)glycine(9),cyclization,Pinner reaction,followed by reaction with n-hexyl chlorofomate.The overall yield is about 40% and the structure of the product was determined by IR,1H NMR and MS.