Iodine-mediated electrocatalysis assist Annulation/cyclization via Intramolecular Benzylic C–H Amination: Batch vs Flow Electrochemistry

The access of heterocyclic compounds via direct amination of C-H bonds are of vital interest because of their role in pharmaceutical and natural products. The combination of molecular iodine and electricity activates benzylic C-H bond and facilitates the amination process via intramolecular C-N bond formation. Iodine works as a mediator for the formation of C-N bond via activation of a distance C-H bond through intermediate N-I bond under electrochemical conditions, so iodine can be called electrocatalyst. Under both batch & flow electrochemistry conditions, similar results were obtained in cyclization product with 77 & 78% yields respectively. However, in case of annulation reaction higher yield was obtained with 99% conversion under flow electrochemical conditions using our design of home-made flow microreactor. In both electrochemical transformations, cyclization as well as annulation reaction, no photocatalyst was used. Notably, flow reactions work under safe & environmentally friendly conditions, and continuous products are obtained.

Water-promoted dehydrative coupling of 2-aminopyridines in heptane via a borrowing hydrogen strategy

We describe a novel strategy for the water-promoted dehydrative coupling reaction in heptane, which offers a sustainable direct amination of alcohols.

Highly economical and direct amination of sp3 carbon using low-cost nickel pincer catalyst

Developing more efficient routes to achieve efficient C–N bond coupling is of great importance to industries ranging from products in pharmaceuticals and fertilizers to biomedical technologies and next-generation electroactive materials.

Origins of ligand-controlled diastereoselectivity in dirhodium-catalysed direct amination of aliphatic C(sp3)–H bonds

The mechanism and origins of ligand-controlled stereoselectivity of dirhodium (Rh2L4, L=OAc, S-tertPTTL)-catalysed intramolecular aliphatic C(sp3)−H aminations have been explored using DFT calculations. Both catalytic cycles occur via the formation of...