Qi Ya-juan
2012
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Journal
Chinese Journal of New Drugs
Abstract
Objective: To study and improve the synthesis proccess of dabigatran etexilate mesylate.Methods: The intermediate ethyl 3-[[3-amino-4-(methylamino)benzoyl](pyridin-2-yl) amino]-propanoate(5) was prepared from 4-methyl amino-3-nitrobenzoic acid(2) and ethyl 3-(pyridin-2-ylamino) propanoate(3) by chlorination,amidation,neutralization and reduction.Dabigatran etexilate mesylate was synthesized from 5 and(4-cyanophenyl) glycine by amidation,cyclization,neutralization,amidination,acylation and salification with methane sulfonic acid.Results: The structures of intermediates and target compound were identified by MS and 1H-NMR.The overall yield was 33.9%.Conclusion: This improved method can be used in industrial manufacturing with the advantage of simpler purifying operation,lower cost and mild condition.