Atherton-Todd反应的研究进展

Recent Advances of the Atherton-Todd Reaction

磷酰胺或磷酸酯类化合物及其衍生物是一类非常重要的含磷有机分子,在药物化学、材料化学以及有机催化等研究领域均有着广泛应用.Atherton-Todd反应是制备这类化合物最有效的方法之一,该反应是指氧磷氢化合物[P(O)-H]在碱的作用下与四氯化碳原位生成磷酰氯[P(O)-Cl]中间体,随后该中间体与醇或胺类化合物反应形成相应的磷酸酯或磷酰胺类化合物及其衍生物.近年来,Atherton-Todd反应由于其操作容易、原子经济性高、底物普适性广以及易于将含磷原子引入到活性化合物结构片段中等优点,受到了合成化学家的广泛关注.总结近几十年来Atherton-Todd反应的研究进展及其在有机合成中的应用,并对目前该领域可能存在的研究挑战提出展望,希望能为Atherton-Todd反应的未来发展方向提供一些借鉴和思考.

Phosphoramides or phosphates and their derivatives are a very important class of phosphorus-containing organic molecules,which are widely applied in medicinal chemistry,material chemistry and organic catalysis.As one of the most effective methods towards constructing phosphorus compounds,the Atherton-Todd reaction involves in situ halogenation of P(O)-H molecules with tetrachloromethane to generate the key intermediates of phosphoryl chlorides in the presence of bases,which subsequently react with amines or alcohols to form the corresponding phosphoramide or phosphate products.In recent years,this reaction has been widely explored by synthetic chemists due to its ease of operation,high atom economy,broad substrate versatility,and ease of incorporation of phosphorus units into active structural fragments.The research progress of the Atherton-Todd reaction and its application in organic synthesis in recent decades are summarized,and a brief outlook on the current research challenges is put forward,hoping to provide reference and thinking for the further development of the Atherton-Todd reaction.