MUMBAI, India, Oct. 31 -- Intellectual Property India has published a patent application (202411024259 A) filed by National Institute Of Pharmaceutical Education And Research, Mohali, Punjab, on March 26, 2024, for 'method of preparation of alogliptin and trelagliptin.'
Inventor(s) include Manjinder Singh Gill; and Divakar Singh.
The application for the patent was published on Oct. 31, under issue no. 44/2025.
According to the abstract released by the Intellectual Property India: "The present invention relates to a six-step process for the synthesis of each alogliptin and trelagliptin. Accordingly, the present invention involves reaction of diphenyl carbonate based synthesis of O-phenyl carbamate in a mixture of organic solvents, followed by synthesis of N-methyl urea by reaction with methyl amine, condensation of N-methyl urea with diethylmalonate ester in the presence of a strong base in an organic solvent to yield 1-methylpyrimidine-2,4,6(1H,3H,5H)-trione which upon halogenation with phosphorus oxychloride yielded 6-chloro-3-methylpyrimidine-2,4(1H,3H)-dione - a common intermediate for the synthesis of alogliptin and trelaglitptin. N-benzylation of 6-chloro-3-methylpyrimidine-2,4(1H,3H)-dione with 2-(bromomethyl)benzonitrile, and reaction with R-3 aminopiperidine yielded alogliptin (I) while N-benzylation of 6-chloro-3-methylpyrimidine-2,4(1H,3H)-dione with 2-(bromomethyl)-4-fluorobenzonitrile, and reaction with R-3 aminopiperidine yielded trelagliptin (II), respectively."
Disclaimer: Curated by HT Syndication.
