Junichiro Yamaguchi, Atsushi D. Yamaguchi, and Kenichiro Itami

Angew. Chem. Int. Ed., 2012, in press. DOI: 10.1002/anie.201201666

The ideal case: The direct functionalization of C–H bonds in organic compounds has recently emerged as a powerful and ideal method for the formation of carbon–carbon and carbon–heteroatom bonds. This Review provides an overview of C–H functionalization strategies for the rapid synthesis of biologically active compounds such as natural products and pharmaceutical targets.