Synthesis of Polysubstituted 3‑Amino Pyrroles via Palladium-Catalyzed Multicomponent Reaction

A novel approach for the synthesis
of polysubstituted 3-amino pyrroles
via palladium-catalyzed three-component tandem reaction was developed.
The procedure constructs various polysubstituted 3-amino pyrroles
with moderate to excellent yields under mild reaction conditions with
assembly efficiency, readily available starting materials, and good
functional group tolerance. Furthermore, this process was successfully
applied to the synthesis of different 3-phenyl-1,4-dihydropyrrolo­[3,2-b]­indole derivatives via an intramolecular Buchwald–Hartwig
cross-coupling reaction in two steps.

本研究开发了一种通过钯催化三组分串联反应合成多取代3-氨基吡咯的新颖方法。该方法可在温和反应条件下，凭借高效的组装过程、易得的起始原料以及良好的官能团耐受性，构建一系列多取代3-氨基吡咯产物，产率处于中等至优异水平。此外，通过两步分子内Buchwald–Hartwig交叉偶联反应，该合成策略可成功应用于多种3-苯基-1,4-二氢吡咯并[3,2-b]吲哚衍生物的制备。