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Isocyanides are well known for their multi-component reactions (MCR), such as the Passerini reaction and the Ugi reaction, with diverse molecular skeletons, high functional group compatibility, and good atom economy. With the continuous research on isocyanides, C(sp3)–H bond functionalization involving isocyanides has made significant progress in recent years. The synergistic combination of isocyanide insertion and C(sp3)–H bond activation offers an effective strategy for the synthesis of various nitrogen- and oxygen-containing compounds and provides an efficient approach for the synthesis of complex molecules in the fields of synthetic chemistry, drug discovery and materials science. This review highlights the recent progress in the C(sp3)–H functionalization involving isocyanides.

Graphical abstract: C(sp3)–H functionalization with isocyanides

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