Sitagliptin is a new class drug for type 2 diabetes. Sitagliptin has two units, b-aminoacid and triazolopyrazine. The synthetic challenge is to the enantioselective construction of the b-aminoacid. The b-hyroxyacid unit has been used as a precursor of b-aminoacid and recently its derivatives were also found to be effective in glycemic control. We aimed to obtain R and S butanoic acid in scalable, simple and mild reaction conditions. We will be discussing our proline catalys enantioselective b-aminoacid synthesis results.

Enantioselective synthesis of (R)- and (S)-b-hydroxyphenylbutanoic acids: Main unit of sitagliptin (Januvia)

244th National Meeting (2012)

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