Exploratory Process Development of Pexidartinib through the Tandem Tsuji-Trost Reaction and Heck Coupling

被引：14

作者：

Chen, Dongsheng ^{[1
,2
]}

Zhang, Yi ^{[1
,2
]}

Li, Jianqi ^{[1
,2
]}

Liu, Yu ^{[1
,2
]}

机构：

[1] China State Inst Pharmaceut Ind, Shanghai Inst Pharmaceut Ind, Novel Technol Ctr Pharmaceut Chem, 285 Gebaini Rd, Shanghai 201203, Peoples R China

[2] China State Inst Pharmaceut Ind, Shanghai Inst Pharmaceut Ind, Shanghai Engn Res Ctr Pharmaceut Proc, 285 Gebaini Rd, Shanghai 201203, Peoples R China

来源：

SYNTHESIS-STUTTGART | 2019年 / 51卷 / 12期

基金：

中国国家自然科学基金;

关键词：

pexidartinib; palladium-silver-catalyzed; tandem; Tsuji-Trost reaction; Heck coupling; HALOGEN-MAGNESIUM EXCHANGE; GIANT-CELL TUMOR; ARYL; MECHANISM;

D O I：

10.1055/s-0037-1612421

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A novel synthetic route to CSF1R inhibitor pexidartinib was designed and demonstrated. Crucial to the successful synthesis is a tandem Tsuji-Trost reaction and Heck coupling in combination with palladium and silver catalysis. The final product was obtained via five steps in 49% yield with purity as high as 99.2%. The cheap and available materials and reagents and easy operations for workup and purification make this route more practical.

引用

页码：2564 / 2571

页数：8

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