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Lin, Kuaile; Cai, Zhengyan; Zhou, Weicheng
Synthetic communications, 12/2013, Letnik: 43, Številka: 24Journal Article
Economic syntheses of sitagliptin phosphate monohydrate, acknowledged as the first dipeptidyl peptidase 4 (DPP-4) inhibitor, have been achieved in an overall yield of 42.4% in four steps from 1-{3-(trifluoromethyl)-5,6-dihydro-1,2,4triazolo4,3-apyrazin-7(8H)-yl}-4-(2,4,5-trifluorophenyl)butane-1,3-dione. The key stereoselective reduction of this process was carried out by NaBH 4 /HCOOH instead of expensive and toxic catalysts or ligands. Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications® for the following free supplemental resource(s): Full experimental and spectral details.
