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3.7.2.1 Sitagliptin: Synthesis of an (R)-Amine by Enzymatic Transamination

DOI: 10.1055/sos-SD-216-00250

Patel, R. N.Science of Synthesis: Biocatalysis in Organic Synthesis, (20153403.

Sitagliptin (2) is an oral antihyperglycemic (antidiabetic drug) of the dipeptidyl peptidase-4 (DPP-4) inhibitor class that is marketed by Merck as Januvia (in the form of the corresponding phosphate salt 3).[‌1‌] It is an enzyme-inhibiting drug that is used for the treatment of diabetes mellitus type 2, either alone or together with other oral antihyperglycemic agents (such as metformin or a thiazolidinedione).

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References