G. Han
2014
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Journal
Drugs and Clinic
Abstract
Objective To study the synthetic technology of dabigatran etexilate. Methods 3-[[[2-[[(4-Cyanophenyl)amino]methyl]-1-methyl-1H-benzimidazol-5-yl]carbonyl] pyridin-2- ylamino]propionic acid ethyl ester was used as starting material to synthesize amidine by Pinner reaction, then to obtain target compound by reacting with hexyl chloroformate. Results The target compound was synthesized and characterized by MS and 1H-NMR. The yield was 38.8% and the purity was 99.6%. Conclusion The synthetic route of dabigatran etexilate has the advantages of simple operation and reasonable design with high yield and purity, and is suitable for industrial production.