Palladium(II)-catalyzed tandem reaction for the assembly of 1,3-disubstituted pyrrolo[1,2-α]pyrazines

Abstract

An efficient and simple synthesis of 1, 3-disubstituted pyrrolo[1, 2-α]pyrazines from substituted 1H-pyrrole- 2-carbonitriles and arylboronic acids was developed. It’s a palladium(II)-catalyzed cascade reaction involving C(sp)–C(sp²) coupling followed by intramolecular C–N bond formation. The method can tolerate various substrates with satisfactory yields.

Graphical Abstract

Keywords:

• pyrrolo[1, 2-α]pyrazine
• C–C coupling
• palladium
• cascade reaction

Additional information

Funding

This research was supported by Zhejiang Provincial Public Welfare Projects under Grant No. LGF22H300002 and Jinhua Science and Technology Projects under Grant No. 2021-3-005.