MUMBAI, India, Sept. 28 -- Intellectual Property India has published a patent application (202511018215 A) filed by Council Of Scientific And Industrial Research An Indian on February 28, 2025, for Improved Synthetic Method For 6-Acetyl-8-Cyclopentyl-5-Methyl-2-Substituent-Pyrido[2,3-D]pyrimidin-7(8h)-One, A Key Intermediate In The Manufacture Of Palbociclib.
Inventors include Indubhusan Deb; Moumita Saha; Koushik Naskar; and Writhabrata Sarkar.
The application for the patent was published on September 25, 2026, under issue no. 39/2026.
Abstract: The present invention offers an environmentally friendly, expensive metal-free, cost-effective, and safe easy to handle synthetic process to synthesize a key intermediate 6-acetyl-2-chloro-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7(8H)-one (E) for the large scale synthesis of Palbociclib. Till date, numerous methods have been developed to synthesize Palbociclib. The current synthesis method of the invention has relatively simple operation, mild reaction conditions, high yield and a simple process. There are several problems in the prevailing synthetic methods for the preparation of Palbociclib, such as the requirement of an expensive Pd metal catalyst, Phosphine ligands, fancy acylating agent, necessity of silver salts to achieve acylation, toxic oxidants, multi-step operation including bromination, and elevated temperature. Notably, a significant gap exists in finding a straightforward, eco-friendly, cost-effective route for synthesizing Palbociclib with high efficacy.
Disclaimer: Curated by HT Syndication.
