Room-Temperature CuI-Catalyzed Amination of Aryl Iodides and Aryl Bromides

A general
and effective CuI/N′,N′-diaryl-1H-pyrrole-2-carbohydrazide
catalyst system was developed for the amination of aryl iodides and
bromides at room temperature with good chemoselectivity between −OH
and −NH2 groups. Only 5 mol % of CuI and ligands
was needed in this protocol to effect the amination of various aryl
bromides and aryl iodides with a wide range of aliphatic and aryl
amines (1.3 equiv).

本研究开发了一种通用且高效的碘化亚铜（CuI）/N',N'-二芳基-1H-吡咯-2-甲酰肼催化体系，可在室温条件下实现芳基碘化物与芳基溴化物的胺化反应，且在羟基（-OH）与氨基（-NH₂）基团间展现出优异的化学选择性。该反应体系仅需5 mol%的碘化亚铜与配体，即可实现各类芳基溴化物、芳基碘化物与多种脂肪胺及芳胺（投料量为1.3当量）的胺化反应。