Copper‐Catalyzed <i>N</i>‐Arylation/Hydroamin(d)ation Domino Synthesis of Indoles and its Application to the Preparation of a Chek1/KDR Kinase Inhibitor Pharmacophore

Abstract

Abstract magnified image Inexpensive copper catalysts allow for efficient syntheses of N ‐aryl‐, N ‐acyl‐, or N ‐H‐(aza)indoles starting from ortho ‐alkynylbromoarenes. The broad scope of this domino N ‐arylation/hydroamin(d)ation process is highlighted by the synthesis of highly functionalized indoles, as well as of a Chek1/KDR inhibitor pharmacophore.