Cheng Huansheng
2013
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Journal
Chinese Journal of Pharmaceuticals
Abstract
In the presence of CDI,the reaction of 4-methylamino-3-nitrobenzoic acid with ethyl 3-(pyridin-2ylamino)propanoate produced ethyl 3-[(4-methylamino-3-nitrobenzoyl)(pyridin-2-yl)amino]propanoate.It was reduced by zinc to afford ethyl 3-[(3-amino-4-methylaminobenzoyl)(pyridin-2-yl)amino]propanoate,which was reacted with [(4-cyanophenyl)amino] acetic acid to give ethyl 3-[[2-[(4-cyanophenylamino)methyl]-1-methyl-1H-benzimidazol5-carbonyl](pyridin-2-yl)amino]propanoate in the presence of CDI,followed by acetic acid in one-pot.Dabigatran etexilate was finally synthesized by amidination and acylation with an overall yield of about 48%.