一、前言 近来我们发现苯骈三氮唑的双活性酰胺除能与胺进行N-酰基化及与醇,酚进行O-酰基化反应外,还具有与羟胺进行选择性N-酰基化反应的能力,即苯骈三氮唑(HBT)的活性酰胺基团,如-COBT是一个很好的、有选择性的脱离基团,它对N-酰基化的反应活性高于其对O-酰基化反应,前反应在无催化剂存在及室温下即可完成,而后反应必须在三乙胺存在下,反应 First, the preface Recently, we found that the bifunctional amide benzotriazole in addition to amine N-acylation and alcohol, phenol O-acylation, but also has a selective N-acylation with hydroxylamine The ability, that is, the active amide group of benzotriazole (HBT), such as -COBT is a good, selective leaving group that is more reactive toward N-acylation than it does to O-acyl The reaction, the pre-reaction in the absence of catalyst and room temperature to complete, and then the reaction must be in the presence of triethylamine, the reaction