Duan Yumin
2010
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Journal
Chinese Journal of Pharmaceuticals
Abstract
3-(Pyridin-2-ylamino)propinoic acid ethyl ester(2) was prepared from 2-chloropyridine by oxidation,substitution and then hydrogenation.4-Methylamino-3-nitrobenzoyl chloride(3) was prepared from 4-chlorotoluene by oxidation,nitration,amination and chlorination.Dabigatran etexilate was synthesized from 2 and 3 by condensation,reduction,amidation,cyclization,amidination and acylation with an overall yield of about 12%(based on 4-chlorotoluene).