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

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 p...

Full description

Saved in:
Bibliographic Details
Published in:Synthesis (Stuttgart) 2019-06, Vol.51 (12), p.2564-2571
Main Authors: Chen, Dongsheng, Zhang, Yi, Li, Jianqi, Liu, Yu
Format: Article
Language:English
Citations: Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:0039-7881
1437-210X
DOI:10.1055/s-0037-1612421