Efficient synthesis of sitagliptin phosphate,a novel DPP-IV inhibitor,via a chiral aziridine intermediate |
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| Authors: | Xianhua Pan Xiaojun Li Qingling Lu Wansheng Yu Weijin Li Qunhui Zhang Fei Deng Feng Liu |
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| Institution: | 1. School of Perfume and Aroma Technology, Shanghai Institute of Technology, 100 Haiquan Rd., Shanghai 201418, PR China;2. Zhejiang Hisoar Pharmaceutical Co., Ltd, 100 Waisha Branch Rd., Jiaojiang, Taizhou, Zhejiang 318000, PR China |
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| Abstract: | Sitagliptin phosphate, a novel DPP-IV inhibitor of T2DM, has been synthesized via 12 linear steps, in an overall yield of 26%. The key step is the coupling reaction of 2,4,5-trifluorophenylmagnesium bromide with a chiral aziridine derivative, which was prepared from l-homo-serine by simple steps. |
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| Keywords: | Sitagliptin phosphate β-Amino acid Grignard reaction Aziridine Synthesis |
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