以四丁基碘化铵(TBAI)为催化剂,过氧叔丁醇(TBHP)作为氧化剂,在温和的反应条件下实现了叔胺氮的邻位碳原子上sp3-C—H键与亚磷酸酯的氧化偶联,反应条件温和,室温、空气下即可进行,适用范围广泛,产率高,后处理方便.为新的C—P键的形成提供了一条简洁高效的反应路径,并且合成了一系列可能具有重要药理和生物活性的α-氨基磷酸酯化合物. Using tetrabutylammonium iodide (TBAI) as catalyst and t-butyl hydroperoxide (TBHP) as oxidant, the sp3-C-H bond on the ortho-carbon atom of tertiary amine nitrogen was reacted under mild reaction conditions with phosphorous acid Ester oxidative coupling, the reaction conditions are mild, room temperature, air can be carried out, a wide range of applications, high yield, post-processing convenience for the formation of a new C-P bond provides a simple and efficient reaction path, and the synthesis A series of α-phosphoramidate compounds, which may have important pharmacological and biological activities,