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Multigram scale, chiron-based synthesis of sacubitril  期刊论文  

  • 编号:
    e5864242-0566-46ee-9abb-27cf78d2f9b1
  • 作者:
    Wang, Yun[1,2] Chen, FenEr[1] Shi, Yong[2] Tian, WeiSheng[2]
  • 语种:
    English
  • 期刊:
    TETRAHEDRON LETTERS ISSN:0040-4039 2016 年 57 卷 52 期 (5928 - 5930) ; DEC 28
  • 收录:
  • 关键词:
  • 摘要:

    Based on a chiron approach, sacubitril, a neprilysin inhibitor and API of Entresto, was synthesized in 7 steps with an overall yield of 40%. Two chiral centers of sacubitril are easily obtained from the starting material, one inherited and another inverted. Noteworthy steps are an efficient and mild preparation of epoxide from chiral vicinal diol using C4F9SO2F/DBU, and a one-flask preparation of succinic amide from azide. All the reactions are performed on multigram scales. (C) 2016 Elsevier Ltd. All rights reserved.

  • 推荐引用方式
    GB/T 7714:
    Wang Yun,Chen Fen-Er,Shi Yong, et al. Multigram scale, chiron-based synthesis of sacubitril [J].TETRAHEDRON LETTERS,2016,57(52):5928-5930.
  • APA:
    Wang Yun,Chen Fen-Er,Shi Yong,Tian Wei-Sheng.(2016).Multigram scale, chiron-based synthesis of sacubitril .TETRAHEDRON LETTERS,57(52):5928-5930.
  • MLA:
    Wang Yun, et al. "Multigram scale, chiron-based synthesis of sacubitril" .TETRAHEDRON LETTERS 57,52(2016):5928-5930.
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