MUMBAI, India, July 31 -- Intellectual Property India has published a patent application (202411101218 A) filed by National Institute Of Pharmaceutical Education And on December 20, 2024, for Efficient Process For Vemurafenib In Three Steps With Water-Based Reactions.
Inventors include Vaishnavi Newaskar; and Sankar Kumar Guchhait.
The application for the patent was published on July 24, 2026, under issue no. 30/2026.
Abstract: The present disclosure relates to a green, efficient, and industrially scalable process for the synthesis of Vemurafenib, an active pharmaceutical ingredient (API) used in cancer treatment. The process comprises three reaction steps: (i) a Suzuki-Miyaura coupling between 5-halo-1H-pyrrolo[2,3-b]pyridine and (4-chlorophenyl)boronic acid in aqueous medium using low catalyst loading; (ii) a Friedel-Crafts acylation employing 3-amino-2,6-difluorobenzoic acid as an acylating agent without prior acid chloride formation; and (iii) sulfonylation of the resulting ketone intermediate with propane-1-sulfonyl chloride in water. The process avoids hazardous reagents and toxic solvents, eliminates protection-deprotection steps, and minimizes the need for chromatographic purification. It operates under mild temperature conditions, offers improved safety and environmental compliance, and achieves a high overall yield of approximately 60%. This greener and cost-effective approach enables a sustainable and scalable route for commercial production of Vemurafenib, reducing India’s dependence on imported APIs and supporting affordable access to oncology therapeutics.
Disclaimer: Curated by HT Syndication.
