Expeditious Access to Functionalized Tricyclic Pyrrolo-Pyridones via Tandem or Sequential C-N/C-C Bond Formations

Org Lett. 2019 Nov 15;21(22):9128-9132. doi: 10.1021/acs.orglett.9b03514. Epub 2019 Nov 7.

Abstract

The facile synthesis of both saturated and unsaturated tricyclic pyrrolo-pyridones starting from a single readily available, common monocyclic reagent has been developed. An intermolecular annulation via a tandem Buchwald-Hartwig/Heck reaction led to the synthesis of β-carbolinones. The analogous semisaturated tricyclic pyrrolo-pyridones were prepared in good to excellent yields by sequential Buchwald-Hartwig and Fischer indole reactions. The methods feature mild reaction conditions and good functional group tolerance.