MUMBAI, India, July 31 -- Intellectual Property India has published a patent application (202411100971 A) filed by National Institute Of Pharmaceutical Education And on December 19, 2024, for Green And Scalable Process For Synthesizing Sorafenib And Regorafenib.
Inventors include Joydev Kumar Laha; Anjali Gupta; and Shubham B Chaudhari.
The application for the patent was published on July 24, 2026, under issue no. 30/2026.
Abstract: The present disclosure relates to a green and transition metal-free process for the preparation of Sorafenib and Regorafenib, two clinically significant antineoplastic agents. The method involves the oxidative carbamoylation of 4-chloro-3-(trifluoromethyl)aniline with semicarbazide to form 1-(4-chloro-3- (trifluoromethyl)phenyl)urea under mild conditions, using tert-butyl hydroperoxide and molecular iodine in aqueous medium. The intermediate is then coupled with substituted anilines to yield diphenyl urea derivatives, which are further reacted with 4-chloro-N-methylpicolinamide in the presence of suitable bases and polar aprotic solvents to afford Sorafenib and Regorafenib in good yields and high purity. The process avoids toxic reagents such as phosgene and isocyanates, and eliminates the need for metal catalysts, offering a cost-effective, environmentally friendly, and industrially scalable alternative. The methodology is consistent with green chemistry principles and offers improved safety, atom economy, and product quality. This synthetic approach is especially advantageous for pharmaceutical industries seeking sustainable API manufacturing solutions.
Disclaimer: Curated by HT Syndication.
