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

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Title: Recent Developments in Microwave-Assisted Metal-Catalyzed C-H Functionalization of Heteroarenes for Medicinal Chemistry and Material Applications.
Authors: Besson, Thierry1, Fruit, Corinne1 corinne.fruit@univ-rouen.fr
Source: Synthesis. 2016, Vol. 48 Issue 22, p3879-3889. 11p.
Subjects: Carbon, Activation (Chemistry), Pharmaceutical chemistry, Irradiation, Microwave heating
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 [ABSTRACT FROM AUTHOR]
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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 [ABSTRACT FROM AUTHOR]
ISSN:00397881
DOI:10.1055/s-0035-1562608