Synthesis of dabigatran etexilate mesylate
QIANG Wen-zhou
HE Kai-min
FU Qiang
Abstract：Objective: To study the synthesis technology of dabigatran etexilate mesylate, and to establish a simple and commercial synthetic procedure. Methods: The intermediate I was synthesized from 4-aminobenzamidine dihydrochloride as starting material, and the intermediate II was synthesized from ethyl 3-(3-amino-4-(methylamino)-N-(pyridin-2-yl) benzamido) propanoate as starting material. The intermediate I and the intermediate II were condensed to synthesize dabigatran etexilate, then to obtain target compound by reacting with mesylate. Results:The target compound was synthesized and confirmed by MS and1 H-NMR. The total yield was 20％ ～ 30％, and the purity was 99. 71％ estimated by HPLC. Conclusion: The synthesis process is simple, reasonable, and has feasibility of industrial production.
Keywords：dabigatran etexilate mesylateprocess researchchemical synthesis
Publication Date：2018-01-01
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：4( 1803-1806 )