Abstract

AbstractAn 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.

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