CC BY 4.0 · SynOpen 2023; 07(03): 422-429
DOI: 10.1055/a-2157-5855
paper

A Practical and Efficient Method for the Synthesis of Sorafenib and Regorafenib

Ramteke Prachi
,
The study was supported by National Institute of Pharmaceutical Education & Research (NIPER), S.A.S. Nagar Punjab (India). Ramteke Prachi thanks NIPER for the award of a scholarship for doctoral studies.


Abstract

Efficient, practical syntheses of sorafenib and regorafenib have been achieved in a manner that is free from the problems associated with previously reported methods. The process involved preparation of 4-(4-aminophenoxy)-N-methylpicolinamide (sorafenib intermediate) and 4-(4-amino-3-fluorophenoxy)-N-methylpicolinamide (regorafenib intermediate) using only a single base and did not require the use of an inert atmosphere. The reaction of intermediates with phenyl 4-chloro-3-(trifluoromethyl)phenyl carbamate, prepared using water-assisted synthesis of carbamates, was used to install the main urea functionality in these molecules.

Supporting Information



Publication History

Received: 17 July 2023

Accepted after revision: 18 August 2023

Accepted Manuscript online:
21 August 2023

Article published online:
26 September 2023

© 2023. This is an open access article published by Thieme under the terms of the Creative Commons Attribution License, permitting copying and reproduction so long as the original work is given appropriate credit. Contents may not be used for commercial purposes or adapted, remixed, transformed or built upon. (https://creativecommons.org/licenses/by/4.0/)

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