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
收藏
页码：2564 / 2571
页数：8
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