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∗
This project was supported from the National Key R & D Program of China (No. 2017YFE0102200), National Natural Science Foundation of China (No. 81673291), and Diabetes National Research Group, USA to Y. Yu.
A direct synthesis of multi-substituted pyrrolo[1,2-a]pyrazines via palladium(II)-catalyzed C(sp)–C(sp2) cascade coupling and intramolecular cyclization in the presence of ligand was developed. This reaction originates from phenylboronic acids and readily synthesized 2-carbonyl- or 2-formylpyrroloacetonitriles, and affords products in good to excellent yields for a diversity of substrates. Additionally, a possible mechanism for the transformation is proposed.
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