高等学校化学学报 ›› 1996, Vol. 17 ›› Issue (8): 1240.

• 论文 • 上一篇    下一篇

含磷稠杂环的合成及其生物活性(Ⅵ)

陆荣健, 刘华银, 杨光富, 杨华铮   

  1. 南开大学国家元素有机化学重点实验室, 南开大学元素有机化学研究所, 天津 300071
  • 收稿日期:1995-08-18 出版日期:1996-08-24 发布日期:1996-08-24
  • 通讯作者: 杨华铮
  • 作者简介:陆荣健,男,33岁,博士,副教授.
  • 基金资助:

    国家自然科学基金;天津市青年科学基金

Synthesis and Bioactivity of Fused Phosphorus Heterocyclic Compounds(Ⅳ)

LU Rong-Jian, LIU Hua-Yin, YANG Guang-Fu, YANG Hua-Zheng   

  1. Naticonal Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071
  • Received:1995-08-18 Online:1996-08-24 Published:1996-08-24

摘要: 在阳离子交换树脂D72存在下5-氨基-3-苄硫基-4-氰基(乙氧羰基)吡唑与苯基二氯化膦和芳醛的类Mannich反应,合成了9个2-苄硫基-3-氰基(乙氧羰基)-5-芳基-6-苯基-6-氧-6-磷杂-4,5,6-三氢咪唑[2,3e]吡唑,利用NMR方法确定其为反式构型,初步研究了反应机制。生物活性测试结果表明,部分化合物具有一定的除草活性。

关键词: 含磷稠杂环, ALS酶抑制剂, 类Mannich反应

Abstract: The Mannich-type cyclizative reaction of 5-amino-3-benzylthio-4-cyano (ethyloxycarbonyl) pyrazole with phenyl phosphonyl dichloride and the aromatic aldehyde in the presence of cation exchange resin D72 was reported.Nine 2-benzylthio-3-cyano (ethyloxycarbonyl)-5-aryl-6-phenyl-6-oxo-6-phospha-4,5,6-trihydroimidazolo[2,3e]pyrazoles were synthesized and identified as trans-configuration by means of1H NMR,31PNMR, The mechanism of the reaction was described.The preliminary biological tests show that some compounds have herbicidal activity.

Key words: Fused phosphorus heterocyclic compound, ALS enzyrne inhibitor, Mannich-type reactoin

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