A Three-Step Synthesis of Acotiamide for the Treatment of Patients with Functional Dyspepsia

被引：3

作者：

Fu, Kai ^{[1
]}

Yang, Liu ^{[1
]}

Wang, Qiu-Fen ^{[1
]}

Zhan, Fu-Xu ^{[1
]}

Wang, Bin ^{[1
]}

Yang, Qian ^{[1
]}

Ma, Zhi-Jia ^{[1
]}

Zheng, Geng-Xiu ^{[1
]}

机构：

[1] Univ Jinan, Sch Chem & Chem Engn, Jinan 250022, Shandong, Peoples R China

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2015年 / 19卷 / 12期

关键词：

STRUCTURE-REACTIVITY CORRELATIONS; CATALYZED HYDROLYSIS; Z-338; SYMPTOMS; TRIAL;

D O I：

10.1021/acs.oprd.5b00256

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

A three-step synthesis of acotiamide is described. The agent is marketed in Japan for treatment of patients with functional dyspepsia. We designed a One-pot method to prepare the key intermediate 5a from 2 via an acyl chloride and amide and then reacted with 6 to obtain 1 under solvent-free condition. With the use of DCC, the unavoidable impurity 5b was also successfully converted into the desired After isolation of 1, we carried forward to the next step of HCl salt formation, which was proved to be a very effective procedure for the removal of practically all major impurities. The process is cost-effective, simple to Operate, and easy to scale-up.

引用

页码：2006 / 2011

页数：6

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