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有机化学
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有机化学 ›› 2001, Vol. 21 ›› Issue (10): 755-758. 上一篇    下一篇

研究论文

3-氰基-2-羟基吡啶磷酸酯的合成

惠琦;常建华;丁贻祥   

  1. 西北大学化学系.西安(710069);中国科学院上海有机化学研究所.上海(200032)
  • 发布日期:2001-10-25

Synthesis of O-(3-cyanopyrid-2-yl) O, O-diethyl phosphorates

Hui Qi;Chang Jianhua;Ding Yixiang   

  1. Northwest Univ, Dept Chem.Xian(710069);Shanghai Inst Organ Chem., CAS.Shanghai(200032)
  • Published:2001-10-25

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β-酮醛和氰乙酰胺在碱的作用下环化得到3-氰基-2-羟基吡啶，用亚磷酸二乙酯在Atherton-Todd条件下磷酰化可以高产率得到3-氰基-2-羟基吡啶磷酸二乙酯，这些化合物显示了一定的生物活性，并可用于磷酸酯酶抑制剂的活性结构的设计。

关键词: 氰基, 磷酰化, 环化, 生物活性, 吡啶P, 磷酸酯, 抑制剂, 磷酸酯酶, 合成

3-Cyano-6-substituted-2-pyridiones generated by cyclization reaction of β-ketonic acid and cyanoacetamide were phophorylated under the Atherton-Todd conditions to give O-(3-cyanopyrid-2-yl) O, O-diethyl phosphorate in good yields. The molecules showed certain bioactivities and would be valuable for the design of phosphatase inhibitors.

Key words: CYANO GROUP, PHOSPHORYLATION, CYCLIZATION, BIOLOGICAL ACTIVITY, PYRIDINE P, PHOSPHATES, INHIBITOR, PHOSPHATASE, SYNTHESIS

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