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What is Enantioselective Synthesis of Sitagliptin about?

This article presents an enantioselective synthesis of (R)-sitagliptin using phase-transfer catalytic aza-Michael addition and Baeyer−Villiger oxidation, achieving 96% enantiomeric excess. The synthesis involves key steps including the reaction of tert-butyl β-naphthylmethoxycarbamate with a specific Michael acceptor, followed by hydrolysis and amide coupling. The overall yield of the synthesis is 41% over seven steps, highlighting the efficiency of the method for producing this important antidiabetic medic

Author

Sangvenkat

Language

EN