高等学校化学学报

高等学校化学学报 ›› 1999, Vol. 20 ›› Issue (9): 1390.

• 论文 • 上一篇    下一篇

不对称1,3,2-苯并二氧磷杂环己烷非对映消旋体的合成及生物活性

成俊然, 文佳, 邵瑞链, 曹焕岩, 黄润秋   

  1. 南开大学元素有机化学研究所, 元素有机化学国家重点实验室, 天津 300071
  • 收稿日期:1998-12-16 出版日期:1999-09-24 发布日期:1999-09-24
  • 通讯作者: 成俊然,女、54岁,副教授.
  • 作者简介:成俊然,女、54岁,副教授.
  • 基金资助:

    天津市自然科学基金(批准号:983602711)资助课题

Synthesis and Biological Activity of Diastereomeric Racemates of Asymmetric 1, 3, 2-Benzodioxaphosphorin Derivatives

CHENG Jun-Ran, WEN Jia, SHAO Rui-Lian, CAO Huan-Yan, HUANG Run-Qiu   

  1. Institute of Elemento-Organic Chemistry, State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, China
  • Received:1998-12-16 Online:1999-09-24 Published:1999-09-24

PDF (PC)

被引次数

4

摘要： 通过相转移催化关环反应合成了新的6-取代-2-疏-2-烷(芳)氧-4-(2,-4二氯苯基)-4-氢-1,3,2-苯并二氧磷杂环已烷(3a-3g),用结晶法分离得到7对非对联消旋体,其结构经1HNMR、31PNMR和元素分析确证,化合物3a-A单晶X射线分析表明其构型为(2R,4S;2S,4R).生物活性测定结果表明,化合物3C有良好的杀虫活性,非对映消旋体A和B具有协同杀虫作用.

关键词: 合成, 1, 3, 2-苯并二氧磷杂环己烷, 非对映消族体, 生物活性

Abstract: New 6-substituted-2-alkoxy (aryloxy)-4-(2, 4-dichlorophenyl)-4H-1, 3, 2-benzodi-oxaphosphorin2-sulfides 3a-3g were synthesized utilizing PTC cyclization reaction.Seven couples of compounds 3a-3g diastereomeric racemates (Aand B) were separated by crystallization.Their structures were confirmed by 1HNMR, 31PNMR and elementary analysis.The single-crystal X-ray analysis of 3a-A indicated that its relative configuration is (2R,4S;2S, 4R).The preliminary bioassays indicate that compound 3c has a good insecticide activity.The diastereomeric racemates Aand Bshow a synergistic insecticide activity.

Key words: Synthesis, 1,3,2-Benzodioxaphosphorin, Diastereomeric racemete, Biological activity

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