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

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