- Synthesis of sitagliptin phosphate by a NaBH4/ZnCl2-catalyzed diastereoselective reduction
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A practical asymmetric synthesis of sitagliptin phosphate, from 1-{3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo-[4,3-a]pyrazin-7(8H)-yl}-4-(2,4,5-trifluorophenyl) butane-1,3-dione, in overall 65.3% yield has been reported. The target compound was synth
- Pan, Xianhua,Wang, Kun,Yu, Wansheng,Zhang, Ruimin,Xu, Lu,Liu, Feng
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p. 1170 - 1172
(2015/09/22)
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- Practical and economical approach to synthesize sitagliptin
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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, 2,4]triazolo[4,3-a]pyrazin-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.]
- Lin, Kuaile,Cai, Zhengyan,Zhou, Weicheng
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supporting information
p. 3281 - 3286
(2013/10/01)
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