Some N¬-acyl-N'-aryl thiourea derivatives 4(a-f) have been prepared by the reaction of acyl halides ammonium thiocyanate and aryl amines. The structures of synthesized compounds have been characterized by IR, 1HNMR spectral studies. The synthesized compounds 5(a-f) have been screened for antibacterial activity. The effect of the structure of the investigated compounds on the antibacterial activ...

Novel N-amino benzylthiolates were synthesized via multicomponent reaction of malononitrile, isothiocyanates and benzyl halides under conventional and solvent-free conditions. Various electron-donating and -withdrawing substitutes within both isothiocyanates and benzyl halides were used to demonstrate the efficiency of new methodology. A broad spectrum of antibacterial and antifungal activities...

A highly efficient copper-catalyzed system using commercially available racemic 1,1′-binaphthyl-2,2′-diol (rac-BINOL) as the ligand was eveloped for amination of aryl halides and heteroaryl halides with alkyl amines and N H heterocycles. Good to high yields were obtained for aryl romides and heteroaryl chlorides. The commercially available rac-BINOL ligand with excellent stability and high effi...

Aminocarbonylation of aryl halides is one of the most useful methods in amide synthesis, but nitroarenes have not been used as a nitrogen source in this method even though they are more economical and accessible than anilines. Reported here is the development of nickel catalysis for the first three-component reactions of aryl halides, Co2(CO)8, and nitroarenes under reductive conditions to prod...

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

The use of FeCl(3) resulted in a fast homocoupling of aryllithiums, and this enabled its integration with the halogen-lithium exchange reaction of aryl halides in a flow microreactor. This system allows the homocoupling of two aryl halides bearing electrophilic functional groups, such as CN and NO(2), in under a minute.

The conversion of aryl halides to phenols under mild reaction conditions is a longstanding and formidable challenge in organic chemistry. Herein, we report the rational design of a broadly applicable Pd-catalyzed method to prepare phenols with benzaldehyde oxime as a hydroxide surrogate. These reactions occur under mildly basic conditions and enable the late-stage hydroxylation of several funct...

An operationally simple iron-catalyzed hydrodehalogenation of aryl halides has been developed with 1 mol% Fe(acac)(3) and commercial t-BuMgCl as reductant. The mild reaction conditions (THF, 0 degrees C, 1.5 h) effect rapid chemoselective dehalogenation of (hetero)aryl halides (I, Br, Cl) and tolerate F, Cl, OR, SR, CN, CO(2)R, and vinyl groups.

We have successfully developed a novel cathodic cross-coupling reaction of aryl halides with arenes. Utilization of the cathodic single electron transfer (SET) mechanism for activation of aryl halides enables the cross-coupling reaction to proceed without the need for any transition metal catalysts or single electron donors in a mild condition. The SET from a cathode to an aryl halide initiates...

A highly efficient Ullmann homocoupling reaction of aryl halides using palladium (II) phosphine-ylide complexes as homogenous pre-catalysts under aerobic conditions has been developed without the need for any chemical co‐reducing agents. The procedure is relatively mild and appears to have broad applicability, being useful for the homocoupling of both electron-deficient and electron-rich aryl h...