Efficient Synthesis of cis ‐3‐Substituted Prolines by Bidentate‐Assisted Palladium Catalysis

A highly effective protocol for the synthesis of C‐3‐substituted prolines has been developed. Pd‐catalyzed C(sp 3 )–H activation is used for the straightforward functionalization of prolines. The use of an 8‐aminoquinolinecarboxamide directing group allows direct arylation, alkenylation, and alkylation at the C‐3 position of prolines in moderate to high yields with diverse iodo‐ or bromo precursors. The resulting 3‐substituted proline derivatives are important units in many biologically active compounds and are useful promoters for a variety of functional group transformations.