4.8 Article

Mechanistic Insights of Copper Catalyzed Trifluoromethyl Aziridine Opening: Regioselective and Stereospecific Aryl Grignard Addition

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Summary: The copper-catalyzed regioselective and stereospecific coupling between aziridines and in situ generated pyridine Grignard reagents is reported in this study. This method enables the synthesis of beta-pyridylethylamines with diverse structures and functionalities, which are potential scaffolds for the synthesis of biologically active compounds commonly found in pharmaceuticals. Additionally, the synthesis of challenging chiral dihydroazaindoles was achieved through mild one-pot reaction conditions involving aziridine opening and nucleophilic cyclization.

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