高等学校化学学报

高等学校化学学报 ›› 1998, Vol. 19 ›› Issue (S1): 186.

• Organic Synthesis Chemistry • 上一篇    下一篇

Synthesis of Novel Derivatives of 1,5-Dihydro-4,6-dithio-l,3,5,2-triazaphosphorine-2-oxide from N,N-bis(2-chloroethyl)diisocyanato phosphoramide

You Huang, Ruyu Chen   

  1. Institute and State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071
  • 出版日期:1998-12-31 发布日期:1998-12-31
  • 基金资助:
    Project 29772018 by National Natural Science Foundation of China

Synthesis of Novel Derivatives of 1,5-Dihydro-4,6-dithio-l,3,5,2-triazaphosphorine-2-oxide from N,N-bis(2-chloroethyl)diisocyanato phosphoramide

You Huang, Ruyu Chen   

  1. Institute and State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071
  • Online:1998-12-31 Published:1998-12-31
  • Supported by:
    Project 29772018 by National Natural Science Foundation of China

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摘要： Cancer is one of the most serious disease of human beings, and studies on antitumor drugs are still challenging scientists to look for new highly active compounds with low toxicity in this field. Cyclophosphamide (Endoxan), one of the most effective antitumor agents has been widely used in cancer chemotherapy1. However, acrolein, from its metabolysis of hepatic mixed function oxidases in the liver, is toxic to the urinary system2, hence,its clinical usage is restricted. With references to our previous works3,4,we designed and synthesized a novel type of compounds Ⅰ with a nitrogen mustard group attached to the phosphorus atom of the heterocyclic ring in which the nitrogen atom at position 5 is from a α-substituted amino acid ester.

Abstract: Cancer is one of the most serious disease of human beings, and studies on antitumor drugs are still challenging scientists to look for new highly active compounds with low toxicity in this field. Cyclophosphamide (Endoxan), one of the most effective antitumor agents has been widely used in cancer chemotherapy1. However, acrolein, from its metabolysis of hepatic mixed function oxidases in the liver, is toxic to the urinary system2, hence,its clinical usage is restricted. With references to our previous works3,4,we designed and synthesized a novel type of compounds Ⅰ with a nitrogen mustard group attached to the phosphorus atom of the heterocyclic ring in which the nitrogen atom at position 5 is from a α-substituted amino acid ester.

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