A methyl sulfonyl radical generated from DMSO in the presence of catalytic Cu(<sc>i</sc>) under O₂atmosphere is used to carry out sulfonation C–C unsaturated bonds afford β-keto sulfones and (<italic>E</italic>)-vinyl sulfones.

An efficient rhodium-catalyzed synthesis of 2H-azirines and pyrroles has been developed. Novel rearrangement α-oximino ketenes derived from α-diazo oxime ethers provides bearing quaternary centers allows for subsequent to highly substituted in excellent yields.

A new strategy to open the 2-allyl-2H-azirines by 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) promotion in metal-free conditions affording 1-azatrienes that situ electrocyclize pyridines good excellent yields is reported. The reaction displays a broad substrate scope and tolerance variety of substituents including aryl, alkyl, heterocyclic groups. In addition, one-pot synthesis from oximes via formation 2H-azirines was achieved.

An efficient dual synthetic manifold for 2-aminofurans and 2-unsubstituted furans has been developed. The carbenoid-mediated [3 + 2] cycloaddition of copper carbenoids with enamines provides 2-amino-2,3-dihydrofurans which serve as common intermediates both furans.

An expedient [5 + 1] annulation method via Rh(III)-catalyzed C–H bond functionalization of enaminones to synthesize polyaromatic rings is described. The reaction tolerates a broad range functional groups and offers new entry construct polycyclic aromatic compounds with amino formyl substituents. A possible mechanism was proposed based on the results obtained from isotope labeling experiments.

A highly site-selective acyloxylation of stable enamines with PhI(OAc)2 under metal-free conditions to afford (E)-vinyl acetate derivatives in good excellent yields is described. Depending on the judicious choice solvent system, either α- or β-site-selective product could be obtained high selectivity. For α-site-selective product, rearranged amide compound as major product. This reaction proceeds mild (room temperature, metal-free, and open-flask) features a broad substrate scope.

We have developed a dual reaction manifold that enables the selective synthesis of both pyridines and pyrroles from common substrates α-diazo oxime ethers.

New bidentate auxiliaries derived from the isoxazole-3-carboxamide and oxazole-4-carboxamide moieties were used for Pd-catalyzed C(sp3)–H bond activation. The results show that, when placed on a primary amine compound, 5-methylisoxazole-3-carboxamide (MICA) directs activation of inert γ-C(sp3)–H bonds C–C formation. Selective efficient arylation alkylation several α-aminobutanoic acid derivatives led to various γ-substituted non-natural amino acids. MICA directing group can be conveniently...

A direct and regiocontrolled thiolation method to access β‐amino sulfides through the palladium‐catalyzed C(sp 2 )–H functionalization of stable enamines was described. The reaction realized under mild conditions by adding an external phosphine ligand prevent poisoning palladium catalyst sulfuric reagents. possible mechanism proposed according obtained results. DFT calculation results were consistent with experiment data, which gave E isomers sulfides. also performed on a gram scale shows...

A cascade strategy to synthesise gem-difluorinated 2H-furans from reactions of BrCF2CO2Et with enaminones has been described. The tolerate a wide variety functional groups under metal-free conditions. An active aminocyclopropane is proposed be key intermediate through the cyclopropanation difluorocarbene enaminones, which further triggers regioselective C-C bond cleavage in situ afford corresponding 2H-furans.

An efficient method to construct functionalized 1,4-ketoaldehydes bearing all-carbon α-quaternary centers<italic>via</italic>regioselective C–C bond activation has been described.

A straightforward strategy for synthesis of highly functionalized trifluoromethyl 2H-furans is described. The copper catalyzed method relies on a cascade cyclic reaction between enaminones and N-tosylhydrazones. This allows the 2-amino-3-trifluoromethyl-substituted 2H-furan derivatives carrying quaternary stereogenic center as single diastereomers. proposed mechanism involves an amino-cyclopropane intermediate formed in cyclopropanation enaminones. developed tolerates broad spectrum...

1,2,4-Thiadiazole derivatives containing a sulfone moiety were designed and synthesized via scaffold hopping to facilitate the discovery of novel antibacterial agents. Most compounds exhibited excellent activity against three plant pathogenic bacteria. The half-maximal effective concentrations (EC50) compound B7 for Xanthomonas oryzae pv (Xoo) X. oryzicola (Xoc) 0.4 1.0 mg/L, respectively. In addition, EC50 values B1 B24 Xoo, Xoc, Pseudomonas syringae actinidiae (Psa) less than 5 mg/L...

The construction of new C–C bonds via inert C(sp 3 )–H bond activation has garnered significant achievements in recent decades, particularly with palladacycles serving as pivotal intermediates.

The skeleton editing strategy has emerged as a transformative approach in drug discovery and agrochemical innovation, enabling precise modifications through the insertion, elimination, or substitution of specific atoms within core carbon heterocyclic frameworks molecules. Recent advancements carbene chemistry have led to significant breakthroughs single‐carbon‐atom insertion reactions, particularly context five‐membered systems. However, application this six‐membered arenes heteroarenes...

Mild catalytic reaction conditions for the synthesis of 2-isoxazolines and 2H-azirines have been developed via carbenoids derived from α-oximino diazo compounds. This has utilized in one-pot pyrroles presence 1,3-dicarbonyl

The phosphonyl radical generated from the reaction of manganese(III) acetate with diethyl phosphonate selectively adds to 3-position flavones and coumarins afford phosphonylated products in moderate good yields.

2H-Azirine-2-caboxamides have been designed to perform as a new type of bifunctional thiol linker under very mild reaction conditions. The cleavage C-N double bond 2H-azirine furnishes an amino amide functional group in situ through addition and ring-opening process. It works with broad scope thiols 2H-azirines the absence any catalysts at room temperature. Cysteine-containing peptides also demonstrated work efficiently completely water solution.

An efficient Au(III)/Ag(I) co-catalytic platform has been established for the synthesis of cyclopentadienes through amine-release annulation enaminones with alkynes. Vinylcarbenoids that were generated from 1,2-migration propargyl esters may undergo a tandem process to give aminocyclopentenes as key intermediates. The bimetal catalytic system is compatible broad substrate scope under mild reaction conditions. obtained are allowed late-stage modifications into complex molecules high chemo-...

An efficient copper catalytic system has been established for the synthesis of highly functional indolizines through oxidative [3 + 2] cycloaddition enamines and pyridotriazoles. This modular platform is compatible with a broad range groups, including natural complex skeletons, allowing late-stage modifications. It features step-economical, regioselective, easy-handling procedure applied in constructing small molecules potent activity toward inhibiting VEGF–NRP1 interaction one-pot reaction...

A one-pot reaction to synthesize functionalized 2H-azirines through visible-light-mediated ring contraction and olefin metathesis of isoxazoles is described. Hoveyda–Grubbs II catalyst was found function as a photocatalyst for these transformations, allowing processes be carried out in manner. This study offers new entry the application Grubbs catalysts efficient photocatalysts possibilities carrying other photoreactions process.

An efficient method to construct azapolycycles via directing group participated benzylic C(sp3)–H/C(sp2)–H cross-dehydrogenative coupling reactions is described. The reaction proceeded through a palladium catalyzed C(sp3)–H activation followed by with C(sp2)–H bond of quinoline afford the azapolycyclic compounds. works broad substrate scope affording products in moderate good yields excellent diastereoselectivities. Control experiments further supported proposed mechanism.

An efficient copper-catalyzed direct C(sp2)–H/C(sp3)–H coupling reaction of aza-aromatic rings with fluoroalcohols is developed. A variety useful building blocks including hydroxyfluoroalkylated aniline, pyrrole, and indole derivatives bearing a quaternary carbon center could be constructed high regioselectivity good to excellent yields under very mild conditions. The believed undergo fluoroalcohol oxidation follow an electronic addition pathway.

This work describes a dual catalytic system for selective synthesis of α-allyl-1,3-ketoaldehydes and α-vinyl-1,4-ketoaldehydes through cascade reactions hydroxyl substituted aromatic enaminones with cyclopropenes under zinc promoted conditions.