高等学校化学学报 ›› 1995, Vol. 16 ›› Issue (8): 1229.

• 论文 • 上一篇    下一篇

N',N'-二-(2-氯乙基)-O-芳基-N3-芳基硫脲基磷酰胺酯的合成、结构及性质研究

陈茹玉, 王惠林, 周嘉   

  1. 南开大学元素有机化学研究所, 天津, 300071
  • 收稿日期:1994-08-27 修回日期:1995-03-18 出版日期:1995-08-24 发布日期:1995-08-24
  • 通讯作者: 陈茹玉,女,74岁,博士,教授(院士).
  • 作者简介:陈茹玉,女,74岁,博士,教授(院士).
  • 基金资助:

    国家自然科学基金

Studies on the Synthesis,Structures and Properties of N',N'-Bis(2-chloroethyl)-O-aryl-N3-aryl Thioureido Phosphoramidate

CHEN Ru-Yu, WANG Hui-Lin, ZHOU Jia   

  1. Institute of Elemento-Organic Chemistry, Nankai University, Tianjin, 300071
  • Received:1994-08-27 Revised:1995-03-18 Online:1995-08-24 Published:1995-08-24

摘要: 合成了14种含有氮芥结构及芳基取代硫脲基的磷酰胺酯,其结构经1HNMR、IR、MS和元素分析证实。研究了它们的波谱性质及结构和化学位移的关系,讨论了磷原子上取代基对反应的影响。初步生测结果表明,部分化合物具有良好的抗TMV病毒活性和良好的抗肿瘤活性。

关键词: 磷酰胺酯, 取代硫脲, 抗病毒剂, 抗肿瘤药物

Abstract: In order to look for novel antitumor drugs and virucides with high activity and low toxicity,a series of the title compounds were synthesized by the addition reaction of N,N-bis( 2-chloroethyl)-O-aryl isothiocyanatido phosphoramidate with aryl amine,and their structures were confirmed by spectroscopic and analytical methods. The relationship between the chemical shifts and structures was revealed. The existence of the intermolecular and intramolecular hydrogen-bondings leads to deshielding and to an increase in the frequency of the NMR signal of the hydrogen-bonded protons. Preliminary bioassays indicate that some of them have good inhibitory effects to the growth of different tumor cells such as BGC,HCT,HL60and BCAP cell lines in human bodies and display a high activity against tobacco mosaic virus(TMV).

Key words: Phosphoramidate, Thioureido, Antivirals, Antitumor agents

TrendMD: