Recent Developments in Microwave-Assisted Metal-Catalyzed C-H Functionalization of Heteroarenes for Medicinal Chemistry and Material Applications

C-C Bond formation from direct C-H activation is now recognized as a powerful and straightforward strategy for the synthesis of complex molecules and especially for late-stage functionalization. Many of these reactions allow a streamlined route to bi(hetero) aryl compounds with applications in medicinal chemistry as well as in organic materials. Since high temperatures and long reaction times are often required for C-H activation, microwave irradiation has emerged as a suitable tool. This short review gives an overview of the metal-catalyzed C-H functionalization of heteroarenes since 2013 and highlights the benefits of microwave irradiation over traditional heating. 1 Introduction 2 Palladium-Catalyzed Direct Functionalization of sp(2) C-H Bonds with Aryl Halides 3 Palladium-Catalyzed and Silver-Assisted Direct Arylation of sp(2) C-H Bonds with Aryl Halides 4 Palladium-Catalyzed and Copper-Assisted Direct Arylation of sp(2) C-H Bonds with Aryl Halides 5 Copper-Catalyzed sp(3)-sp(2) C-C Bond Formation 6 Conclusion