Abstract

AbstractC−H bond functionalization is one of the most efficient strategies for the rapid synthesis of cyclic amines containing substituents in the ring, which are core structures of many bioactive molecules. However, it is much more challenging to perform this strategy on remote C−H bonds than on α‐C−H bonds of cyclic amines. This review provides a comprehensive overview on the transition metal‐free methods for the remote C−H bond functionalization of cyclic amines, complementary to methods relying on transition metal catalysis. Selected substrate scope and discussion of reaction mechanism are given when necessary.

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