Abstract Iron catalysis has been developed for the intermolecular 1,2‐addition of perfluoroalkyl iodides to alkynes and alkenes. The a wide substrate scope high functional‐group tolerance. A variety including CF 3 I can be employed. resulting perfluoroalkylated alkyl alkenyl further functionalized by cross‐coupling reactions. This methodology provides straightforward streamlined access organic molecules.

Abstract Esters are one of the most common functional groups in natural and synthetic products, one-step conversion ester group into other is an attractive strategy organic synthesis. Direct amidation esters particularly appealing due to omnipresence amide moiety biomolecules, fine chemicals, drug candidates. However, efficient methods for direct unactivated still lacking. Here we report nickel-catalysed reductive coupling with nitroarenes furnish step a wide range amides bearing relevant...

Abstract (Hetero)Aryl amines, an important class of organic molecules in medicinal chemistry, are most commonly synthesized from anilines, which turn by hydrogenation nitroarenes. Amine synthesis directly nitroarenes is attractive due to improved step economy and functional group compatibility. Despite these potential advantages, there yet no general method for the (hetero)aryl amines carbon–nitrogen cross-coupling Here we report reductive coupling with alkyl halides yield amines. A simple...

Selective catalytic synthesis of Z-olefins has been challenging. Here we describe a method to produce 1,2-disubstituted olefins in high Z selectivity via reductive cross-coupling alkyl halides with terminal arylalkynes. The employs inexpensive and nontoxic catalyst (iron(II) bromide) reductant (zinc). substrate scope encompasses primary, secondary, tertiary halides, the reaction tolerates large number functional groups. utility is demonstrated several pharmaceutically relevant molecules....

A nickel-catalysed reductive aminocarbonylation of (hetero)aryl halides employing readily available nitro(hetero)arenes as the nitrogen source has been developed.

Amides are an important class of organic compounds, which have widespread industrial applications. Transamidation amides is a convenient method to generate new from existing ones. Tertiary amides, however, challenging substrates for transamidation. Here we describe unconventional approach the transamidation tertiary using nitroarenes as nitrogen source under reductive conditions. Manganese metal alone mediates reactions and no additional catalyst required. The exhibits broad scope high...

Transmidation is an attractive method for amide synthesis. However, transamidation of secondary amides challenging. Here, we describe a reductive that employs readily available nitro(hetero)arenes as the nitrogen sources, zinc or manganese reductant, and simple nickel salt ligand catalyst system. The scope includes both alkyl aryl amides, with high functional group compatibility.

A copper(II)-catalyzed oxidative cyclization of enamides to oxazoles via vinylic C–H bond functionalization at room temperature is described. Various 2,5-disubstituted bearing aryl, vinyl, alkyl, and heteroaryl substituents could be synthesized in moderate high yields. This reaction protocol complementary our previously reported iodine-mediated afford 2,4,5-trisubstituted oxazoles.

A general method for the Pd-catalyzed coupling of methanol with (hetero)aryl halides is described. The reactions proceed under mild conditions a wide range aryl and heteroaryl to give methyl ethers in high yield.

A method for the Pd-catalyzed arylation of ammonia with a wide range aryl and heteroaryl halides, including challenging five-membered heterocyclic substrates, is described. Excellent selectivity monoarylation to primary arylamines was achieved under mild conditions or at rt by use bulky biarylphosphine ligands (L6, L7, L4) as well their corresponding aminobiphenyl palladacycle precatalysts (3a, 3b, 3c). As this process requires neither glovebox nor high pressures ammonia, it should be widely...

A simple protocol for iron-catalyzed cross-coupling of nonactivated secondary alkyl bromides and iodides with alkynyl Grignard reagents at room temperature has been developed. wide range halides terminal alkynes are tolerated to afford the substituted in good yields. slight modification reaction also allows a variety primary halides.

A method for the hydroxylation of aryl and heteroaryl halides, promoted by a catalyst based on biarylphosphine ligand tBuBrettPhos (L5) its corresponding palladium precatalyst (1), is described. The reactions allow cross-coupling both potassium cesium hydroxides with (hetero)aryl halides to afford variety phenols hydroxylated heteroarenes in high excellent yield.

Abstract Iron catalysis has been developed for the intermolecular 1,2‐addition of perfluoroalkyl iodides to alkynes and alkenes. The a wide substrate scope high functional‐group tolerance. A variety including CF 3 I can be employed. resulting perfluoroalkylated alkyl alkenyl further functionalized by cross‐coupling reactions. This methodology provides straightforward streamlined access organic molecules.

Aryl diazonium salts occupy a privileged role in synthetic chemistry owing to their ready availability and versatile reactivity. While applications accessing diversely functionalized arene derivatives via denitrogenation‐coupling reduction/addition reactions have been well recognized by practitioners both academia industry, recent renaissance chemical transformations of retaining the key N 2 ‐unit has emerged as powerful technique construct various ‐heterocycles. This review covers history...

<italic>N</italic>-Aryl amides were synthesized <italic>via</italic> the manganese-mediated amidation of esters with nitroarenes without need for additional catalysts or ligands.

Transamidation has recently emerged as a straightforward and convenient means to diversify amides. However, the kinetically thermodynamically demanding transamidation of notoriously robust, fully alkyl-substituted tertiary amides still remains longstanding challenge. Here, we describe method for activation alkyl streamline using simple tungsten(VI) chloride catalyst chlorotrimethylsilane an additive. The highly electrophilic oxophilic tungsten enables selective scission C–N bond effect...

We describe the base-mediated [3 + 2] cycloaddition reaction of di/trifluoromethylated hydrazonoyl chlorides with fluoronitroalkenes for synthesis densely functionalized 3-di/trifluoroalkyl-5-fluoropyrazoles potent biological activity.

The stereoselective synthesis of trisubstituted alkenes is challenging. Here, we show that an iron-catalyzed anti-selective carbozincation terminal alkynes can be combined with a base-metal-catalyzed cross-coupling to prepare in one-pot reaction and high regio- stereocontrol. Cu-, Ni-, Co-based catalytic systems are developed for the coupling sp-, sp(2) -, sp(3) -hybridized carbon electrophiles, respectively. method encompasses large substrate scope, as various alkynyl, aryl, alkenyl, acyl,...

N-Aryl amides are an important class of compounds in pharmaceutical and agrochemical chemistry. Rapid low-cost synthesis N-aryl remains high demand. Herein, we disclose operationally simple process to access directly from readily available nitroarenes carboxylic acids as coupling substrates. This method involves the situ activation acyloxyphosphonium salt for one-pot amidation, without need isolation corresponding synthetic intermediates. Furthermore, ease preparation workup allow quick...

Alkyl N-aryl 1,2,3-triazole-carboxylates are important molecules or intermediates in medicinal chemistry, but the synthesis of N2-aryl counterparts remains elusive. Herein, we describe a Cu-mediated annulation reaction alkyl 3-aminoacrylates with aryldiazonium salts, both which readily available substrates. Furthermore, 2-aminoacrylates also viable Diverse and their analogues can be rapidly prepared under mild conditions. Especially, this protocol allows one to access several druglike...

Ni metal-mediated aminocarbonylation based on readily available arylboronic acids, nitroarenes, and carbon monoxide was achieved to prepare a variety of aryl amides.

The unified construction of cyano-substituted 1,2,4-triazoles, particularly the 5-cyano counterparts, remains underdeveloped. Herein we describe a three-component method to access wide range 1-aryl 5-cyano-1,2,4-triazoles using readily available 2-diazoacetonitriles, nitriles, and aryldiazonium salts. This regiospecific synthesis relies on dipolar [3 + 2] annulation in situ formed nitrile ylides with Furthermore, this protocol can be amendable gram-scale synthesis, chemical transformations...

Perceived pain intensity is an important determinant of health-related quality life. A lack studies has investigated the co-influences physical and psychosocial risk factors on perceived shifts in effects after pandemic. As a post-COVID symptom, it to re-assess for heath care. Four dimensions physical/psychosocial were assessed: medical history, personal wellbeing psychological distress, lifestyle, socio-demographic characteristics. We first identified subgroups with significant increase...

Direct <italic>N</italic>-formylation of nitroarenes with CO₂ is developed to prepare <italic>N</italic>-aryl formamides without the need preforming anilines as conventional substrates.