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As an emerging method for the direct asymmetric functionalization of C(sp3)–H bonds, the asymmetric [1,5]-hydride transfer reactions have received considerable attention in recent years. The remarkable features of these reactions include their redox-neutral nature and facile access to versatile polycyclic scaffolds when coupled with the downstream cyclization process. Thanks to the continuous efforts in this field, an array of effective catalytic systems such as chiral organocatalysts, Lewis acids, and binary acid catalysts that are capable of promoting asymmetric [1,5]-hydride transfer reactions has been identified. This chapter will focus on providing a concise description of the state-of-the-art of this exciting area.

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