Synthesis of 2,3,5-trisubstituted 1H-pyrroles via formal [3 + 2] cycloaddition of 1-arylpropynes and nitriles and their antiproliferative activities

Abstract

A straightforward approach for the assembly of 2,3,5-trisubstituted 1H-pyrroles via a base-mediated [3 + 2] cycloaddition of 1-arylpropynes with nitriles has been reported through alkali metal salt-promoted C(sp³)–H functionalization. This reaction features a transition metal-free catalyst, facile starting materials and a wide substrate scope. Moreover, the biological evaluation revealed that these pyrrole products exhibit antiproliferative activities against MDA-MB-231, SGC-7901, and HCT-116 cells, which provides potential applications in pharmaceutical chemistry.