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2.5 C—C Bond Formation by Double C—H Activation

DOI: 10.1055/sos-SD-218-00066

Xia, J.-B.; You, S.-L.Science of Synthesis: Catalytic Transformations via C—H Activation, (20152115.

General Introduction

This chapter focuses on transition-metal-catalyzed aryl—aryl bond-forming reactions via double C—H activation. Biaryl scaffolds have received much attention as a privileged structure broadly found in biologically active natural products, pharmaceuticals, agrochemicals, and functional molecules in material sciences, etc.[‌1‌,‌2‌] Several general methods have been developed to synthesize biaryls. Traditional methods such as the Ullmann reaction,[‌3‌] the Scholl reaction,[‌4‌] and the Gomberg–Bachmann reaction[‌5‌] are very useful but the substrate scope is limited. Recently developed transition-metal-catalyzed cross-coupling reactions have proved to be efficient for the synthesis of biaryls, generally in high yields and with excellent selectivity and broad substrate scope.[‌6‌]

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