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Stereoselective Synthesis of Dipeptidyl Peptidase-4 (DPP-4) Inhibitor, (R)-Sitagliptin

Ramisetti Anjibabu,Jagan Mohan Reddy Boggu,Putta Shekhar,Basi V. Subba Reddy

CHEMISTRYSELECT（2016）

Cited 7|Views2
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Abstract
An operationally simple and efficient strategy for a highly potent Dipeptidyl Peptidase-4 (DPP-4) inhibitor, sitagliptin has been developed employing readily available precursors. The chiral beta-amino acid core of sitagliptin has been constructed through a Barbier type allylation of chiral sulfinyl imine or a Mannich type addition of diethyl malonate. This approach is more convenient, exquisitely selective and practical.
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Key words
Barbier type of allylation,Mannich reaction Sitagliptin,tert-butanesulfinamide
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