Brønsted acidic ionic liquid as an efficient and reusable catalyst for one-pot synthesis of 1-amidoalkyl 2-naphthols under solvent-free conditions

A mild and efficient method has been developed for the preparation of amidoalkyl naphthols from condensation of aldehydes with amides or urea and 2-naphthol in the presence of a catalytic amount of Brønsted acidic ionic liquid ([TEBSA][HSO₄]) under thermal solvent-free conditions. High yields, short reaction time, easy work-up and reusability of the catalyst are advantages of this procedure.     

A new one-pot neat synthesis of 1,2,4-triazol-3-ones through 4-（N,N-dimethylamino） pyridine （DMAP） catalyzed cyclocondensation of ethyl carbazate with aryl nitriles

A new one-pot neat synthesis of some 5-aryl-2,4-dihydro-3H- 1,2,4-triazol-3-ones through cyclocondensation of ethyl carbazate with aryl nitriles catalyzed by DMAP as an efficient and basic nucleophilic catalyst is described.     

Microwave-assisted one-pot synthesis of 3-substituted-3,4-dihydrocoumarins via tendem Konevenagel and Hantzsch reactions

A convenient route for the synthesis of 3,4-dihydrocoumarin derivates from salicylaldehyde derivates and 1,3-dicarbonyl compounds under solvent-free microwave irradiation conditions was described. In this way, a range of compounds was obtained in moderate to good yields in a short reaction time.     

Efficient one-pot synthesis of substituted 2-amino-1,3,4-oxadiazoles

A convenient one-pot method for the preparation of substituted 2-amino-1,3,4-oxadiazoles has been developed. The method is a significant improvement over previously reported syntheses. Reaction of carboxylic acids with thiosemicarbazides afforded the corresponding oxadiazoles in moderate to good yields. In general, the products precipitated from the reaction mixture, and were collected by filtration. In most of the cases, no chromatographic separations were required. To explore the scope and limitations of this reaction, various aliphatic, aromatic, and heteroaromatic carboxylic acids were reacted with different substituted thiosemicarbazides. The influence of R¹ and R² substituents on the reaction yield and additional results demonstrating the versatility of this method are presented.     

Ultrasound-assisted one-pot three-component synthesis of new isoxazolines bearing sulfonamides and their evaluation against hematological malignancies

In the present study, following a one-pot two-step protocol, we have synthesized novel sulfonamides-isoxazolines hybrids (3a-r) via a highly regioselective 1,3-dipolar cycloaddition. The present methodology capitalized on trichloroisocyanuric acid (TCCA) as a safe and ecological oxidant and chlorinating agent for the in-situ conversion of aldehydes to nitrile oxides in the presence of hydroxylamine hydrochloride, under ultrasound activation. These nitrile oxides could be engaged in 1,3-dipolar cycloaddition reactions with various alkene to afford the targeted sulfonamides-isoxazolines hybrids (3a-r). The latter were assessed for their antineoplastic activity against model leukemia cell lines (Chronic Myeloid Leukemia, K562 and Promyelocytic Leukemia, HL-60).     

Synthesis of 2-substituted 4,5-dihydro-4-oxo-3-furancarboxylates using acylative intramolecular cyclization of sulfonium salts

A simple and efficient synthesis of 4,5-dihydro-4-oxo-3-furancarboxylates using an acylative intramolecular cyclization of sulfonium salts is described. The reaction involved the efficient formation of a mixed anhydride between a linear carboxylic acid and trifluoroacetic anhydride in the presence of N-methylimidazole, followed by the sequential conversion into a highly reactive acylammonium species in situ. This procedure is easily handled, uses readily available inexpensive reagents, and provides a variety of 2-substituted 4,5-dihydro-4-oxo-3-furancarboxylates.     

Efficient synthesis of aryl-substituted carbazoles via tandem double or triple suzuki coupling and cadogan cyclization

An efficient one-step method to prepare aryl-substituted carbazoles via tandem double or triple CC bond formations by multiple Suzuki couplings and CN bond formation by Cadogan cyclization has been developed. The developed method employs commercially available or easily preparable polybromonitrobenzenes and arylboronic acids as starting materials, tolerates various functional groups, and provides good yields.     

Synthesis of new 3-cyanoacetamide pyrrole and 3-acetonitrile pyrrole derivatives

A new fused heterocyclic derivatives of pyrrole containing acetonitrile or cyanoacetonitrile moiety at 3-position is described by a one-pot multicomponent reaction. The reaction of dimedone, various aniline, aryl glyoxal with malononitrile/ethyl cyanoacetate/methyl cyanoacetate under mild conditions. The present method does not involve any hazardous organic solvents or catalysts. The significant features of this method are readily available starting materials, good yields, and easy purification.     

Sequential reactions from catalytic hydroformylation toward the synthesis of amino compounds

Different families of new amino compounds were efficiently synthesized, through optimized sequential processes, involving rhodium catalyzed hydroformylation as the key step. The selection of appropriate hydroformylation catalytic systems and reaction conditions allowed obtaining aldehydes derived from several n-alkyl olefins, cholest-4-ene and 3-vinyl-1H-indole, which were subsequently transformed, in one-pot, in to α-amino acids via hydroformylation/Strecker reaction, and in to tertiary amines via hydroaminomethylation, with excellent yields.     

One-pot synthesis of highly functionalized pyrano[2,3-c]pyrazole-4,4′-diacetate and 6-oxo-pyrano[2,3-c]pyrazole derivatives catalyzed by urea

A facile one-pot, multicomponent protocol for the synthesis of 1,4-dihydro-pyrano[2,3-c]pyrazole derivatives using a urea catalyst is reported. This transformation proceeds via a four-component reaction of ethyl acetoacetate, a hydrazine, 3-oxo-pentanedioic acid dimethyl ester, and malononitrile. The bifunctional nature of urea means that it catalyzes many steps in this transformation, including domino Knoevenagel condensation, Michael addition, and ring opening and closing reactions. This synthetic method has several advantages, including good yield, simple work-up, harmless by-products, and simple purification.