Synthesis 2016; 48(22): 3879-3889
DOI: 10.1055/s-0035-1562608
short review
© Georg Thieme Verlag Stuttgart · New York

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

Thierry Besson
Normandie Univ, UNIROUEN, INSA Rouen, CNRS, COBRA, 76000 Rouen, France   Email: [email protected]
,
Corinne Fruit*
Normandie Univ, UNIROUEN, INSA Rouen, CNRS, COBRA, 76000 Rouen, France   Email: [email protected]
› Author Affiliations
Further Information

Publication History

Received: 28 June 2016

Accepted: 29 June 2016

Publication Date:
22 August 2016 (online)


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

 
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