A new pathway via intermediate 4-amino-3-fluorophenol for the synthesis of regorafenib
A practical synthetic route to regorafenib, in which the target compound was obtained via a 10-step synthesis starting from 2-picolinic acid, 4-chloro-3-(trifluoromethyl)aniline, and 3-fluorophenol, is reported. Crucial to the strategy is the preparation of 4-amino-3-fluorophenol via Fries and Beckman rearrangements using an economical and practical protocol. The main advantages of the route include inexpensive starting materials and an acceptable overall yield. A scale-up experiment was carried out to provide regorafenib with 99.96% purity in 46.5% total yield.
Du, Fangyu,Zhou, Qifan,Shi, Yajie,Yu, Miao,Sun, Wenjiao,Chen, Guoliang
supporting information
p. 576 - 586
(2019/02/01)
A practical synthesis of 2'-fluoro-4'-hydroxyacetophenone
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Zhang, Xiao-Bo,Lu, Qun,Xu, Wei-Ming
experimental part
p. 419 - 421
(2009/12/24)
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