One-Pot Synthesis of Enantiopure Pyrrolopiperazines

A simple one-pot protocol for the synthesis of fused pyrrolopiperazines with a complete diastereoselectivity has been developed. This novel methodology combined the Ugi reaction with a spontaneous enamine alkylation on a multicomponent domino reaction, starting from nonprotected diamines and arylglyoxals.

本研究开发了一种具备完全非对映选择性的稠合吡咯并哌嗪（fused pyrrolopiperazines）合成一锅法方案。该新型方法将乌吉反应（Ugi reaction）与自发烯胺烷基化结合至多组分多米诺反应体系中，以未保护的二胺与芳基乙二醛作为起始原料。