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Optically active 5‐aryl 2,5‐disubstituted pyrrolidines are the principal structural moiety of many bioactive compounds including natural products and catalysts for asymmetric synthesis. A highly regio‐ and diastereoselective and enantiospecific method for direct CH arylation of aliphatic amine has been developed. Structurally diverse enantiopure arylated pyrrolidines were synthesized from commercially...
The oxidative coupling of primary amines with internal alkynes catalyzed by Ru complexes is presented as a general atom‐economy methodology with a broad scope of applications in the synthesis of N‐heterocycles. Reactions proceed through regioselective CH bond activation in 15 minutes under microwave irradiation or in 24 hours with conventional heating. The synthesis of 2,3,5‐substituted pyridines,...
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