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Palladium(II)-Catalyzed C(sp)-C(sp2) Coupling: A Direct Approach to Multi-Substituted Pyrrolo[1,2-a]pyrazines

Chang He, Zijuan Wang, Yitong Chen, Guolin Zhang*, Yongping Yu*

*College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, P. R. of China, Email:,

C. He, Z. Wang, Y. Chen, G. Zhang, Y. Yu, Synthesis, 2021, 53, 2051-2056.

DOI: 10.1055/s-0040-1706644

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A palladium(II)-catalyzed C(sp)-C(sp2) coupling of phenylboronic acids and readily synthesized 2-carbonyl- or 2-formylpyrroloacetonitriles followed by intramolecular cyclization provide multisubstituted pyrrolo[1,2-a]pyrazines in very good yields.

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Key Words

C-C coupling, palladium, cascade reactions, fused N-heterocycles, substituted pyrrolo[1,2-a]pyrazines

ID: J66-Y2021