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Classic synthetic organic chemistry mainly utilizes highly reactive chemical bonds. In contrast, the development of synthetic reactions using less reactive chemical bonds has attracted much attention. This is due to the academic challenge of cleaving strong chemical bonds with low reactivity and the move toward new innovations from conventional synthetic methods. Central to this trend is the activation of C–H bonds. Many challenges must be overcome, however, to directly utilize less-reactive C–H bonds in synthetic organic chemistry. This chapter presents a brief review of the history of developing transformations in which C–H bond activation is a key step. Also, this chapter honors the tremendous efforts that have made C–H bond activation a useful synthetic organic reaction.

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