高等学校化学学报 ›› 1997, Vol. 18 ›› Issue (12): 1992.

• 论文 • 上一篇    下一篇

N-对甲苯磺酰基-α-氨基膦酸及其单酯的合成及活性研究

戴庆, 陈茹玉   

  1. 南开大学元素有机化学研究所, 天津 300071
  • 收稿日期:1996-10-28 出版日期:1997-12-24 发布日期:1997-12-24
  • 通讯作者: 戴庆, 男, 28岁, 博士.
  • 作者简介:戴庆, 男, 28岁, 博士.
  • 基金资助:

    国家自然科学基金

Synthesis of(N-p-Tolueneslfonyl)α-aminobenzylphjosphonic Acid and Its Monoesters and Their Biological Activities

DAI Qing, CHEN Ru-Yu   

  1. Institute of Elemento-Orga,lic Chemistry, Nankai University, Tianjin 300071
  • Received:1996-10-28 Online:1997-12-24 Published:1997-12-24

摘要: 31PNMR谱跟踪反应的方法,研究了对甲苯磺酷胺与取代苯甲醛及三氯化磷(或烷氧基二氯化磷)在乙酸氯为溶剂的条件下的类Mannch反应的机理,找到了合成标题化合物的简单方法.初步生物活性测试表明其中某些化合物具有较好的抗烟草花叶病毒活性.

关键词: &alpha, -氨基膦酸, 类Mannich反应, 反应机理, 烟草花叶病毒

Abstract: The titIe compounds were synthesized by the Mannich-type reactions involving p-toluenesulfonamide, various aromatic aldehydes and alkoxydichlorophosphine (phosphorus-trichloride) in acetyl chloride and subsequent hydrolysis.The reaction mechanism was sug-gested according to the results of 31P NMRtracing reactions- The bioassays showed thatsome of the products possess potential anti-TMVactivity.

Key words: α-Aminophosphonic acid, Mannich-type reaction, reaction mechanism, TMV

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