We describe the one-pot direct N-acylation of indazole with carboxylic acids using DMAPO/Boc2O system. This system is simple and provides N1-acyl indazoles in high yield with high N1 selectivities. This new method ...
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Copper‐Catalyzed Fluoroamide‐Directed Remote C(sp3)‐H Bond Functionalization Through Intramolecular Hydrogen Atom Transfer
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In the recent years, copper-catalyzed fluoroamide-directed remote C(sp3)-H bond functionalization via intramolecular HAT has served as a robust and elegant strategy for the assembly of a variety of functionalized (sulfon)amides and related derivatives. This review focuses on the recent advances in this area. These transformations usually exhibit high efficiency, excellent selectivities and good functional group compatibility.
Abstract
Direct C−H functionalization is an important strategy for the rapid synthesis of valuable organic molecules. Radical-involved remote C(sp3)-H functionalization based on hydrogen atom transfer (HAT) becomes an important method enabling selective direct transformation of C(sp3)-H bonds at specific distal position(s). In the recent years, copper-catalyzed fluoroamide-directed remote C(sp3)-H bond functionalization through intramolecular HAT has served as a robust and elegant strategy for the assembly of a variety of functionalized (sulfon)amides and related derivatives. This review focuses on the recent advances in this area. These transformations proceed effectively with high selectivities and good functional group compatibility under mild conditions.
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