In Situ Generation of Propadiene from 1-Cyclopropyl-1-nitrosourea for Rh(III)-Catalyzed Synthesis of Isoquinolinones and Pyridinones Containing a Methylene Functionality

Org Lett. 2023 Apr 28;25(16):2771-2776. doi: 10.1021/acs.orglett.3c00596. Epub 2023 Apr 14.

Abstract

A Rh(III)-catalyzed synthesis of isoquinolinones and pyridinones bearing a methylene motif is presented. This protocol using easily accessible 1-cyclopropyl-1-nitrosourea as the precursor of propadiene features simple and practical manipulation and tolerates a broad spectrum of functional groups, including strong coordinating N-containing heterocyclic substituents. Late stage diversification and the rich reactivity of methylene for further derivations demonstrate the value of this work.