3‐Acylquinolines possess widespread applications in functional chemicals. However, the convenient and selective synthesis of such important substructures has to date remained a challenge. Herein, we report a method to access 3‐acylquinolines from α, β‐unsaturated ketones and 2‐aminoaryl alcohols in one pot with a copper nanocatalyst supported on nitrogen‐silica‐doped carbon (Cu/N−SiO2−C). Mechanistically, the construction of the product involves a cascade procedure including radical‐type oxidation of 2‐aminoaryl alcohols, aza‐Michael addition and annulation. This developed protocol proceeds with merits of mild reaction conditions, good functional group tolerance, earth‐abundant and reusable copper catalyst, easily available stocks and O2 as the sole oxidant, which provides an alternative way for the sustainable synthesis of quinoline derivatives.

Herein, a method to access 3-trifluoromethyl-1,4-benzoxazines from CF3-imidoyl sulfoxonium ylides and 2-bromophenols has been demonstrated. This synthetic protocol proceeds in a one-pot two-step sequence including lithium-bromide-promoted O-H insertion of sulfoxonium...

Herein, a new strategy for the direct synthesis of functionalized pyrroles from β-amino alcohols and ynones via ruthenium-catalyzed acceptorless dehydrogenative coupling has been demonstrated. This developed methodology proceeds in an...