Copper-Catalyzed Bifunctionalization/Annulation of Unactivated Alkene with Alkyl Bromides

β-Lactam is a ubiquitous scaffold in bioactive compounds and pharmaceuticals. Herein, we disclose a streamlined method for the construction of β-lactams starting from unactivated alkenes and alkyl bromides via a Cu-catalyzed inter-/intramolecular carboamidation. This reaction proceeded smoothly under mild reaction conditions and exhibited a broad substrate scope and various functional groups. This protocol is not only compatible with 1, 2, and 3° alkyl bromides but also suitable for α-bromo nitrile as well as various benzyl bromides. The mechanism exploration indicated that sequential radical addition/reductive elimination was involved

Synthesis of Difluoroarymethyl-Substituted Benzimidazo[2,1‑<i>a</i>]isoquinolin-6(5<i>H</i>)‑ones under Mild Conditions

A highly efficient method for synthesis of difluoroarymethyl-substituted benzimidazo­[2,1-a]­isoquinolin-6­(5H)-ones using 2-arylbenzoimidazoles with α,α-difluorophenylacetic acid as reaction substrates has been developed through radical cascade cyclization. The advantage of this strategy lies in excellent functional group tolerance to generate the corresponding products in good yields under base- and metal-free conditions

Synthesis of Difluoroarymethyl-Substituted Benzimidazo[2,1‑<i>a</i>]isoquinolin-6(5<i>H</i>)‑ones under Mild Conditions

A highly efficient method for synthesis of difluoroarymethyl-substituted benzimidazo­[2,1-a]­isoquinolin-6­(5H)-ones using 2-arylbenzoimidazoles with α,α-difluorophenylacetic acid as reaction substrates has been developed through radical cascade cyclization. The advantage of this strategy lies in excellent functional group tolerance to generate the corresponding products in good yields under base- and metal-free conditions

Palladium-Catalyzed C8‑H Acylation of 1‑Naphthylamines with Acyl Chlorides

A facile and efficient protocol for palladium-catalyzed regioselective C8-H acylation of 1-naphthylamine derivatives with acyl chlorides has been developed. The reaction exhibits broad functional group tolerance, and both aromatic and α,β-unsaturated acyl chlorides can be effectively coupled with 1-naphthylamines. Moreover, the picolinamide moiety as a bidentate directing likely plays a key role in this regioselective transformation

Iridium-Catalyzed Direct C–H Sulfamidation of Aryl Nitrones with Sulfonyl Azides at Room Temperature

Ir­(III)-catalyzed direct C–H sulfamidation of aryl nitrones has been developed to synthesize various sulfamidated nitrones in moderate to excellent yields with excellent regioselectivity and broad functional group tolerance. This transformation could proceed smoothly at room temperature with low catalyst loading in the absence of external oxidants, acids, or bases. Molecular nitrogen was released as the sole byproduct, thus providing an environmentally benign sulfamidation process. And this protocol could efficiently apply to synthesize the substituted benzisoxazoline via one-step transformation from the product

“One-Pot” Approach to 8‑Acylated 2‑Quinolinones via Palladium-Catalyzed Regioselective Acylation of Quinoline <i>N</i>‑Oxides

A “one-pot” facile and efficient protocol for 8-acylated 2-quinolinones has been developed through palladium-catalyzed acylation of quinoline <i>N</i>-oxides, which proceeds with high selectivity at the C8-position. The desired products were isolated in up to 95% yield and good functional group tolerance. A palladacycle was isolated from the catalytic process and proposed as a key intermediate

C8-Selective Acylation of Quinoline <i>N</i>‑Oxides with α‑Oxocarboxylic Acids via Palladium-Catalyzed Regioselective C–H Bond Activation

A facile and efficient protocol for palladium-catalyzed C8-selective acylation of quinoline <i>N</i>-oxides with α-oxocarboxylic acids has been developed. In this approach, <i>N</i>-oxide was utilized as a stepping stone for the remote C–H functionalization. The reactions proceeded efficiently under mild reaction conditions with excellent regioselectivity and broad functional group tolerance

“One-Pot” Approach to 8‑Acylated 2‑Quinolinones via Palladium-Catalyzed Regioselective Acylation of Quinoline <i>N</i>‑Oxides

A “one-pot” facile and efficient protocol for 8-acylated 2-quinolinones has been developed through palladium-catalyzed acylation of quinoline <i>N</i>-oxides, which proceeds with high selectivity at the C8-position. The desired products were isolated in up to 95% yield and good functional group tolerance. A palladacycle was isolated from the catalytic process and proposed as a key intermediate

Iridium-Catalyzed Direct C–H Sulfamidation of Aryl Nitrones with Sulfonyl Azides at Room Temperature

Ir­(III)-catalyzed direct C–H sulfamidation of aryl nitrones has been developed to synthesize various sulfamidated nitrones in moderate to excellent yields with excellent regioselectivity and broad functional group tolerance. This transformation could proceed smoothly at room temperature with low catalyst loading in the absence of external oxidants, acids, or bases. Molecular nitrogen was released as the sole byproduct, thus providing an environmentally benign sulfamidation process. And this protocol could efficiently apply to synthesize the substituted benzisoxazoline via one-step transformation from the product

“One-Pot” Approach to 8‑Acylated 2‑Quinolinones via Palladium-Catalyzed Regioselective Acylation of Quinoline <i>N</i>‑Oxides

A “one-pot” facile and efficient protocol for 8-acylated 2-quinolinones has been developed through palladium-catalyzed acylation of quinoline <i>N</i>-oxides, which proceeds with high selectivity at the C8-position. The desired products were isolated in up to 95% yield and good functional group tolerance. A palladacycle was isolated from the catalytic process and proposed as a key intermediate