Transition Metal-Catalyzed Direct Arylation of Substrates with Activated sp³-Hybridized C−H Bonds and Some of Their Synthetic Equivalents with Aryl Halides and Pseudohalides

C‐2 Arylation of Piperidines through Directed Transition‐Metal‐Catalyzed sp3 CH Activation

“…[1] While the direct functionalization of sp 2 C À H bonds is an active field of research, [2] the corresponding knowledge on sp 3 C À H bonds is still limited and remains one of the current challenges in organic chemistry. [3] Within the area of sp 3 CÀH activation, the transformation of a CÀH bond in the a-position to the nitrogen atom of saturated cyclic amines is of particular importance, [4] since such heterocyclic motifs can be found in an impressive number of natural products and marketed drugs. [5] The intermolecular, direct transition-metal-catalyzed functionalization of saturated cyclic amines adjacent to nitrogen offers a simple and efficient synthetic approach towards valuable building blocks.…”

Exploiting the C-H bond in metal catalyzed C-C bond forming reactions

“…This area is much more challenging since it turned out that aliphatic C-H bonds are much harder to activate in a selective manner as compared to aromatic ones. [57][58][59] This is reflected in literature as well where much more contributions on C(sp 2 )-rather than C(sp 3 )-H activation are reported. Our focus was on direct arylation methods of cyclic and acyclic amines and we have contributed to this field with several protocols.…”

α-Functionalization of Carbonyl Compounds Using Hypervalent Iodine Reagents

“…There are several metal-catalyzed methods to accomplish α-arylation using aryl halides, but these routes suffer from high temperatures, long reaction times and drawbacks associated with the use of heavy metals in industry. [2,99] Diaryliodonium salts and other hypervalent iodine reagents provide a means by which α-arylation can be achieved without the need for toxic or expensive transition metal reagents.…”