An unprecedented direct reductive amination of electron-deficient amines such as Cbz-, Boc-, EtOCO-, Fmoc-, Bz-, ArSO2-, Ar2PO-, etc. protected amines with aldehydes is achieved using the Re2O7 catalyst and silanes as the hydride source. Excellent regioselective mono-alkylation and chemoselective reductive-amination were observed.
首次实现了采用Re2O7催化剂和
硅烷作为氢源,对Cbz-、Boc-、EtOCO-、Fmoc-、Bz-、ArSO2-、Ar2PO-等电子不足的
胺类保护基胺与醛的直接还原胺化反应。观察到优异的区域选择性单烃基化和
化学选择性还原胺化。