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Asymmetric Construction of a Multi-Pharmacophore-Containing Dispirotriheterocyclic Scaffold and Identification of a Human Carboxylesterase 1 Inhibitor  期刊论文  

  • 编号:
    030a57f6-6c74-439a-b614-797e4bfa8098
  • 作者:
    Bao, Xiaoze#[1]Wei, Shiqiang[1];Qian, Xingkai[2]Qu, Jingping[1];Wang, Baomin*[1]Zou, Liwei*[2]Ge, Guangbo[2]
  • 语种:
    英文
  • 期刊:
    ORGANIC LETTERS ISSN:1523-7060 2018 年 20 卷 11 期 (3394 - 3398) ; JUN 1
  • 收录:
  • 摘要:

    A catalytic asymmetric [3 + 2] cyclization of novel 4-isothiocyanato pyrazolones and isatin-derived ketimines was developed, delivering a wide range of intriguing dispirotriheterocyclic products in high yield with excellent diastereoselectivity and enantioselectivity. A chiral sulfoxide derivative of this dispirocyclic product was identified to be a promising hit of the human carboxylesterase 1 inhibitor, and the significant difference of the activity between two enantiomers emphasized the importance of this asymmetric process.

  • 推荐引用方式
    GB/T 7714:
    Bao Xiaoze,Wei Shiqiang,Qian Xingkai, et al. Asymmetric Construction of a Multi-Pharmacophore-Containing Dispirotriheterocyclic Scaffold and Identification of a Human Carboxylesterase 1 Inhibitor [J].ORGANIC LETTERS,2018,20(11):3394-3398.
  • APA:
    Bao Xiaoze,Wei Shiqiang,Qian Xingkai,Qu Jingping,&Ge Guangbo.(2018).Asymmetric Construction of a Multi-Pharmacophore-Containing Dispirotriheterocyclic Scaffold and Identification of a Human Carboxylesterase 1 Inhibitor .ORGANIC LETTERS,20(11):3394-3398.
  • MLA:
    Bao Xiaoze, et al. "Asymmetric Construction of a Multi-Pharmacophore-Containing Dispirotriheterocyclic Scaffold and Identification of a Human Carboxylesterase 1 Inhibitor" .ORGANIC LETTERS 20,11(2018):3394-3398.
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