A fast and site-selective biaryl synthesis via dehydrogenative C–H/C–H arylation in a ball mill was developed. In this paper, both electron-deficient oximes electron-rich anilides quickly under mild conditions provided with various arenes to give the products high-level selectivity. Given solventless mechanochemical conditions, transformation obviated use of large amounts arene coupling partners as solvents allowed utilization more-complicated more-expensive partners, which may dramatically...

A facile and site-selective C–H bond fluorination of phenols using removable 2-pyridyloxy group as an auxiliary was developed. Alternatively, late-stage bioactive 2-phenoxyl nicotinate derivatives diflufenican were also feasible under the present strategy.

Abstract Selective introduction of fluorine into molecules by the cleavage inert C−H bonds is central academic and synthetic interest, yet remains challenging. Given role alcohols in organic chemistry as most ubiquitous building blocks, a versatile selective C(sp 3 )−H 2 fluorination simple alcohols, enabled novel designed exo ‐directing groups, described. bond was achieved using acetone oxime auxiliary, whereas new, modular easily accessible bidentate auxiliary developed for efficient...

A novel palladium catalyzed highly para-selective C-H difluoromethylation of electron-deficient aromatic carbonyls was developed. Diverse substituted ketones and benzoates were selectively difluoromethylated at the remote para-site carbonyl groups in moderate to good yields. Moreover, difuoromethylation also compatible with several complex bioactive molecules.

A versatile and site-selective nitrate-promoted C-H bond fluorination using various weak coordinating amides as intrinsic directing groups was developed. Diverse tertiary secondary underwent selective aromatic fluorination, which features broad substrate scope, good regioselectivity, mild conditions. Moreover, the late-stage of challenging benzeneacetamides via distal reported for first time.

Selective C(sp3)–C(sp2) bond construction is of central interest in chemical synthesis. Despite the success classic cross-coupling reactions, cross-dehydrogenative coupling between inert C(sp3)–H and C(sp2)–H bonds represents an attractive alternative toward new bonds. Herein, we establish a selective inter- intramolecular arylation alcohols with nondirected arenes that thereby provides general pathway to access wide range β-arylated alcohols, including tetrahydronaphthalen-2-ols...

<title>Abstract</title> Aliphatic amines, such as N,N-dialkyl secondary are important chemical entities in biologically active compounds. The regio- and stereoselective C-H functionalisation of acyclic amines therefore great interest importance. Among the possible approaches, radical-mediated via hydrogen atom transfer (HAT) has emerged powerful strategy to access elaborated amines. However, despite recent advances, controllable regio-divergent enantioselective bond transformation at...

A detailed mechanism study on the anion ligand promoted selective C–H bond fluorination is reported.

The direct aromatic C–H bond fluorination of ketones was developed for the first time, providing a short alternative to access anacetrapib through late-stage fluorination.

A palladium catalyzed selective C(sp3)-H arylation and acetoxylation of alcohols using a practical bidentate auxiliary were developed. Masked selectively arylated at the β-position with diverse aryl iodides for first time. Moreover, an efficient site-selective various primary methyl, methylene, benzylic bonds was performed by cheap K2S2O8 as external oxidant.

Herein we report a novel Cu-catalyzed regioselective C2-H alkylation of benzimidazoles with aromatic alkenes. The reaction features exclusive regioselectivity and broad substrate scope in the intermolecular terminal internal alkenes, constituting modular access toward benzimidazole-containing 1,1-di(hetero)aryl alkanes. intramolecular alkenes has been achieved an endo-selective manner. enantioselective C2 also realized moderate to good stereocontrol.

The aromatic C–H bond etherification with alcohols is one of the most atom-efficient ways to construct aryl ethers. However, it often requires a large excess as reagents, which limits substrate scope (especially for valuable alcohols). Herein, an alternative mechanochemical oximes diverse primary and secondary was developed first time. Given solvent-less condition ball milling technique, amount used in this chemistry has been significantly reduced (1.5–3.0 equiv substrates), thus enabling...

A novel Ni-catalysed deamidative fluorination of twist amides with electrophilic fluorinating reagents is reported, affording diverse acyl fluorides in good yields.

A novel strategy was developed for the modular synthesis of CH₂F-containing ketones through palladium catalysed β-selective methyl C(sp³)–H fluorination.

A practical and concise approach for the synthesis of β-aryl amides γ-aryl amines has been developed by utilizing innate carbonyl native as valid coordinating groups.

Abstract Selective introduction of fluorine into molecules by the cleavage inert C−H bonds is central academic and synthetic interest, yet remains challenging. Given role alcohols in organic chemistry as most ubiquitous building blocks, a versatile selective C(sp 3 )−H 2 fluorination simple alcohols, enabled novel designed exo ‐directing groups, described. bond was achieved using acetone oxime auxiliary, whereas new, modular easily accessible bidentate auxiliary developed for efficient...

A novel fluoroarylation of gem -difluorostyrenes with AgF and (hetero)arenes through a Pd( ii )-catalysed C(aryl)–H activation cascade was developed, constituting an efficient method to access CF 3 -substituted fluorenes 1,1-diarylmethanes.

Mechanochemistry has received increasing attention in the past decade.Among which, mechanochemical C-H bond functionalization emerged as a hot research topic.In comparison with traditional solution-based organic reactions, transformation features solvent-less conditions and short reaction time, constituting green efficient synthetic method modern chemical society.Notably, given outstanding features, some long-standing challenges previous reactions could be well-solved by methods.Therefore,...

The synthesis of stereo-defined α-trifluoromethyl arylenes is great importance in medical chemistry, organic and materials science. However, despite the recent advances, Z-selective formation has remained underdeveloped. Here, we describe a facile approach towards Z-α-trifluoromethyl through Pd-catalysed stereoselective fluoroarylation 1,1-difluoroallenes presence bulky monophosphine ligand.

A nitrate-promoted Pd-catalysed cross-dehydrogenative C(sp²)–H oxidation of oximes or azobenzenes with diverse aromatic and aliphatic acids was developed, allowing the versatile formation <italic>O</italic>-aryl esters under mild reaction conditions.