Synthesis of Polysubstituted Pyrroles via (2 + 2 + 1) Cyclization of Enone Oxime Ethers with Alkynes and Diaziridinone
Abstract
Herein, we report an efficient palladium-catalyzed (2 + 2 + 1) cyclization strategy for the synthesis of polysubstituted pyrroles from enone oxime ethers, alkynes, and diaziridinone. This transformation is proposed to proceed through a cascade process involving C-C bond cleavage, migratory insertion of alkyne into the C-Pd bond, C-H activation, and subsequent amination with diaziridinone. Notably, this protocol enables the direct incorporation of bioactive fragments into the pyrrole skeleton, highlighting its synthetic utility in medicinal chemistry applications.
Fields of Study & Subjects
Catalytic C–H Functionalization Methods
Synthesis and Catalytic Reactions
Synthesis and Characterization of Pyrroles
Publication details
- Journal / source
- The Journal of Organic Chemistry
- Publisher
- American Chemical Society (ACS)
- Volume
- 91
- Issue
- 3
- Pages
- 1271–1275
- Publication date
- 10 January 2026
- Language
- EN