Rhodium-Catalyzed Azine-Directed C-H Amidation with -Methoxyamides.

Using -methoxyamide reagents as an amide source, C-H amidation was realized at the ortho position of azine under the action of rhodium and boric acid. The method has mild reaction conditions, high atomic utilization, excellent yield, and wide adaptability to amidation reagents (both aromatic amides and fatty amides are applicable). Amide-substituted ketones can be obtained by a simple treatment and can be further transformed into bioactive substances.

Rhodium-Catalyzed C(sp)-H Amidation of Azine with Sulfonamides.

Direct C-H amidation of azine with sulfonamide was developed for the first time. The reactions proceeded smoothly under benign conditions and gave the corresponding products with high selectivity. This approach shows high regioselectivity, wide substrate scope, and functional group tolerance.