Direct (Hetero) arylation Reactions of (Hetero) arenes as Tools for the Step-and Atom-Economical Synthesis of Biologically Active Unnatural Compounds Including Pharmaceutical Targets

摘要

The significant number of papers and reviews published in this last decade testifies to the utility of the transition-metal-catalyzed direct C-H (hetero)arylation reactions of (hetero)arenes as efficient and powerful tools for the step-and atom-economical, regio- and chemoselective synthesis of natural and unnatural compounds. However, no review has so far been devoted to summarizing the application of these reactions in the synthesis of biologically active compounds. This review with 341 references aims to fill this gap, providing a comprehensive picture of the transition-metal-catalyzed intra-and intermolecular direct C-H (hetero) arylation reactions of (hetero) arenes with (hetero) aryl halides or pseudohalides that have been used as key steps of syntheses of unnatural biologically relevant compounds including pharmaceutical targets, up to the end of September 2015. Attention has also been directed to provide a brief description of the biological properties of the synthesized compounds.