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有机化学
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有机化学 ›› 2010, Vol. 30 ›› Issue (02): 285-288. 上一篇    下一篇

研究简报

手性1-芳基-2-(1H-1,2,4-三唑-1-基)乙醇衍生物的合成与生物活性

徐胜臻1，明志会1，杨娇艳2，杨邵2，丁明武*,1，肖文精*,1   

  1. (1华中师范大学农药与化学生物学教育部重点实验室 武汉 430079)
    (2华中师范大学生命科学院 武汉 430079)
  • 收稿日期:2009-06-24 修回日期:2009-08-26 发布日期:2010-02-20
  • 通讯作者: 肖文精 E-mail:wxiao@mail.ccnu.edu.cn
  • 基金资助:

    国家级.国家自然科学基金

Synthesis and Biological Activities of Enantioriched 1-Aryl-2-(1H-1,2,4-triazol-1-yl)ethanols

Xu Shengzhen1 Ming Zhihui1 Yang Jiao-yan2 Yang Shao2 Ding Mingwu*,1 Xiao Wenjing*,1   

  1. (1 Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, Central China Normal University, Wuhan 430079)
    (2 College of Life Sciences, Central China Normal Uni-versity, Wuhan 430079)
  • Received:2009-06-24 Revised:2009-08-26 Published:2010-02-20

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被引次数

1

取代苯乙烯1与KHSO5在手性催化剂2存在的条件下反应, 生成1-芳基环氧化物3, 3与1H-1,2,4-三唑在固体碳酸钾催化下作用, 得到手性的1-芳基-2-(1H-1,2,4-三唑-1-基)乙醇衍生物4. 部分4对甾醇14α-脱甲基化酶表现出强结合作用.

关键词: 三唑, 手性, 14α-脱甲基化酶, 抑菌活性

Substituted styrene 1 was reacted with KHSO5 in the presence of the chiral catalyst 2 to give aryloxiranes 3, which were subsequently treated with 1H-1,2,4-triazole and potassium carbonate to generate enantioriched 1-aryl-2-(1H-1,2,4-triazol-1-yl)ethanols 4. Some of the triazoles 4 exhibited strong binding interactions with the cytochrome P450-dependent sterol 14α-demethylase (CYP51).

Key words: triazole, chiral, 14α-demethylase, fungicidal activity