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

Abstract

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 sp² C–H Bonds with Aryl Halides

3 Palladium-Catalyzed and Silver-Assisted Direct Arylation of sp² C–H Bonds with Aryl Halides

4 Palladium-Catalyzed and Copper-Assisted Direct Arylation of sp² C–H Bonds with Aryl Halides

5 Copper-Catalyzed sp³-sp² C–C Bond Formation

6 Conclusion

Key words

C–H arylation - microwave irradiation - palladium - heteroarenes - medicinal chemistry - materials - C–C bond formation

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