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The application of exo-type directing groups (DGs) has led to the discovery of a wide range of novel C(sp3)–H activation methods, which allow efficient and site-selective functionalization of alcohol and amide derivatives. In this mini-review we discuss the challenges of this field and summarize the achievements, including DG designs, reaction discoveries and mechanistic studies.

Graphical abstract: sp3 C–H activation via exo-type directing groups

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