报道了利用金催化与铜催化相结合合成5-氨基-2H-吡咯的方法.首先通过均相金催化异恶唑与炔酰胺反应生成α-亚胺金卡宾中间体,再经[3+2]环加成反应合成并分离出5-氨基-3H-吡咯,然后通过铜催化的去酰基化和基团迁移反应来实现3H-吡咯向2H-吡咯的转化.该方法不但操作简单、反应条件温和、官能团兼容性良好,而且还能进行克量级放大.这项研究为合成具有重要生物活性的5-氨基-2H-吡咯化合物提供了广谱实用的合成方法. A method for the synthesis of 5-amino-2H-pyrrole using gold catalysis coupled with copper catalysis was reported.At first, the isoxazole was reacted with alkynylamide to form the α-imine gold carbene intermediate through homogeneous metal catalysis, followed by [3 + 2 ] Cycloaddition reaction to synthesize 5-amino-3H-pyrrole and then convert the 3H-pyrrole to 2H-pyrrole through copper-catalyzed deacylation and group transfer reaction.The method not only has the advantages of simple operation, good reaction conditions Mild, good functional group compatibility, but also can be magnified in grams .This study provides a broad spectrum of practical synthesis methods for the synthesis of 5-amino-2H-pyrrole compounds with important biological activity.