MUMBAI, India, June 30 -- Intellectual Property India has published a patent application (202541101950 A) filed by Cocreate Global Technologies Private Limited on October 23, 2025, for A Novel And Cost-Effective Process For The Synthesis Of (±) Cyclopentane Pyrazole Derivative Intermediate Of Lenacapavir.
Inventors include Tapan Kumar Jena; Prem Kumar Begari; Dipak Bhosale; Jagan Mohan Charry; Ravi Ponniah; Javed Iqbal; and Joseph M. Fortunak.
The application for the patent was published on June 26, 2026, under issue no. 26/2026.
Abstract: An alternative and highly efficient synthetic process for the preparation of the cyclopentane pyrazole derivative intermediate of Lenacapavir is disclosed. The process utilizes inexpensive starting materials and a reduced number of synthetic steps compared to prior art methods. The synthesis involves the sequential steps of acetoxylation of a cyclopentenone derivative, Corey-Chaykovsky cyclopropanation to form a cyclopropane derivative, and difluorination using diethylaminosulfur trifluoride (DAST). The difluorinated intermediate is then subjected to hydrolysis and oxidation to yield a keto derivative, which undergoes condensation with ethyl trifluoroacetate and a final cyclization reaction with a hydrazine ethyl ester derivative to yield the key bicyclic intermediate. The inventive process provides a cost- effective and scalable route, addressing the need for a more accessible manufacturing process for the life-saving HIV drug.
Disclaimer: Curated by HT Syndication.
