A Facile Method for the Synthesis of Betrixaban-Reference-Cited by-同舟云学术

A Facile Method for the Synthesis of Betrixaban

Published:2015-09 Issue:9 Volume:39 Page:524-526
ISSN:1747-5198
Container-title:Journal of Chemical Research
language:en
Short-container-title:Journal of Chemical Research

Author:

Li Jianye¹,Chen Ligong²,Yan Xilong²,Li Yang²,Wei Daiyan¹,Wang Donghua¹

Affiliation:

1. School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, P.R. China

2. School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, P.R. China

Abstract

A facile method for the synthesis of N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide (Betrixaban) from 5-methoxy-2-nitrobenzoic acid is achieved by reduction, acylation, chlorination, acylation and the formation of the amidine. A dechlorinated impurity is avoided in this method. Using tetrahydrofuran as the solvent in the four steps makes its recovery easier. The total yield of the target compound is about 40% and this method is suitable for large-scale production.

Publisher

SAGE Publications

Subject

General Chemistry

Link

http://journals.sagepub.com/doi/pdf/10.3184/174751915X14400926401559

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