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

摘要

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 β-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.