Synthesis ( IF 2.2 ) Pub Date : 2019-04-01 , DOI: 10.1055/s-0037-1612421 Dongsheng Chen 1, 2 , Yi Zhang 1, 2 , Jianqi Li 1, 2 , Yu Liu 1, 2
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Abstract
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.
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.
中文翻译：
通过串联Tsuji-Trost反应和Heck偶联探索Pexidartinib的探索性工艺开发
抽象的
设计并证明了一种新的合成途径来合成CSF1R抑制剂pexidartinib。成功合成的关键是串联的Tsuji-Trost反应和与钯和银催化结合的Heck偶联。通过五个步骤以49％的收率获得最终产物，纯度高达99.2％。廉价和可用的材料和试剂以及易于进行后处理和纯化的操作使该路线更加实用。
设计并证明了一种新的合成途径来合成CSF1R抑制剂pexidartinib。成功合成的关键是串联的Tsuji-Trost反应和与钯和银催化结合的Heck偶联。通过五个步骤以49％的收率获得最终产物，纯度高达99.2％。廉价和可用的材料和试剂以及易于进行后处理和纯化的操作使该路线更加实用。
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