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. Additionally, this transformation can also be scaled up to the gram level. This strategy allows for the direct preparation of ortho-sulfonamide-substituted ketone products, thus providing a good complement to previous C−H amidation.

Using N-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. This provides a good supplement for the C–H bond amidation of aromatic rings.

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An efficient and convenient synthetic strategy for Ruthenium (II)-catalyzed ortho-acylation of N-(2-pyridyl)-anilines using α-oxycarboxylic acids as acyl sources is described. The procedure can be smoothly proceeded under mild conditions, showing...

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