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DOI: 10.1055/a-2157-5855
A Practical and Efficient Method for the Synthesis of Sorafenib and Regorafenib
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
- Supporting information for this article is available online at https://doi.org/10.1055/a-2157-5855.
- 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. The Author(s). 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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