Azirine-enabled regioselective synthesis of N -alkyl pyrazoles and indole–pyrazole conjugates via Cu-catalysed N–N bond formation
Abstract
-alkyl pyrazoles in good to excellent yields under mild, operationally simple, and ambient conditions. The strategy efficiently accommodates aliphatic amines and α-amino esters, delivering aliphatic pyrazoles with comparable efficiency. Moreover, the synthesis of novel classes of indole-pyrazole conjugates underscores the versatility of this approach. This protocol avoids hazardous reagents and harsh conditions, offering a practical alternative to conventional pyrazole synthesis. The broad substrate scope and synthetic utility of this method, exemplified by the rapid access to drug-like scaffolds, highlight its potential application in medicinal chemistry.
Fields of Study & Subjects
Synthesis and Catalytic Reactions
Catalytic C–H Functionalization Methods
Catalytic Cross-Coupling Reactions
Publication details
- Journal / source
- Organic & Biomolecular Chemistry
- Publisher
- Royal Society of Chemistry (RSC)
- Volume
- 24
- Issue
- 21
- Pages
- 4477–4487
- Publication date
- 1 January 2026
- Language
- EN