MUMBAI, India, July 31 -- Intellectual Property India has published a patent application (202411102250 A) filed by National Institute Of Pharmaceutical Education And on December 23, 2024, for A Process For The Preparation Of Aminocarbonylated Phenylalanine Derivatives.
Inventors include Anku Sharma; and Rahul Jain.
The application for the patent was published on July 24, 2026, under issue no. 30/2026.
Abstract: The present invention relates to aminocarbonylated phenylalanine derivatives and a process for the preparation of the same thereof using a palladium-catalyzed aminocarbonylation reaction. The method involves coupling of protected halogenated phenylalanine methyl esters with primary or secondary amines in the presence of an ex-situ generated carbon monoxide source. The carbon monoxide is produced by the hydrolytic cleavage of chloroform using a strong base in a separate chamber and is subsequently diffused into the reaction chamber. The process enables regioselective and stereochemically conserved formation of amide bonds under mild conditions without the use of hazardous CO gas. The method is compatible with a wide variety of amines and phenylalanine derivatives, offering good yields and operational simplicity. The invention is particularly useful for late-stage functionalization of peptides and synthesis of non-natural amino acids. The described process is scalable, economical, and suitable for pharmaceutical and synthetic applications involving modified amino acid intermediates.
Disclaimer: Curated by HT Syndication.
