3-Alkyl(Aryl)-4-amino-4,5-dihydro-1H-1,2,4-triazol-5-ones (2) reacted with 2-furoyl chloride and thiophene-2-carbonyl chloride to afford the corresponding 3- alkyl(aryl)-4-(2-furoylamino)-4,5-dihydro-1H-1,2,4-triazol-5-ones (3) and 3-alkyl(aryl)- 4-(2-thienylcarbonylamino)-4,5-dihydro-1H-1,2,4-triazol-5-ones (4), respectively. The new compounds synthesized were characterized by using IR, 1H-NMR...

The reaction of 3-aryl-N-(aryl)propiolamides with arenes in TfOH at room temperature for 0.5 h led to 4,4-diaryl-3,4-dihydroquinolin-2-(1H)-ones in yields of 44-98%. The obtained dihydroquinolinones were further transformed into the corresponding N-acyl or N-formyl derivatives. For the latter, the superelectrophilic activation of the N-formyl group by TfOH in the reaction with benzene resulted ...

Conformational properties of N-aryl-1-azacyclooctan-5- ones with a p-methyl, m-methyl, and p-methoxy group as a substituent have been studied by 1H-NMR, 13C-NMR and IR spectroscopies. Transannular interaction of the two functional groups have been examined from the ring inversion barriers and the carbonyl vibrational frequencies with reference to the corresponding data...

today, the bidentate ligands 3-hydroxypyridin-4-ones (hpos) as orally active iron chelating agents have been demonstrated to possess potential for treatment of some human diseases such as iron-overload in thalassaemic patients and malaria. in this research, a series of hpos with different substitutes and position were theoretically invest

The synthesis of 5-substituted 6,6a-dihydroisoindolo[2,1-a]quinolin-11(5H)-ones via [4 + 2] imino-Diels-Alder cyclization from N-aryl-3-hydroxyisoindolinones and N-vinyl lactams under Lewis acid-catalysed anhydrous conditions is reported. Reactions of N-(2-substituted-aryl)-3-hydroxyisoindolinones with N-vinylpyrrolidone under identical conditions resulted in the formation of 2-(2-substitued-ar...

Tankyrases-1 and -2 (TNKS-1 and TNKS-2) have three cellular roles which make them important targets in cancer. Using NAD(+) as a substrate, they poly(ADP-ribosyl)ate TRF1 (regulating lengths of telomeres), NuMA (facilitating mitosis) and axin (in wnt/β-catenin signalling). Using molecular modelling and the structure of the weak inhibitor 5-aminoiso quinolin-1-one, 3-aryl-5-substituted-isoquinol...

Today, the bidentate ligands 3-hydroxypyridin-4-ones (HPOs) as orally active iron chelating agents have been demonstrated to possess potential for treatment of some human diseases such as iron-overload in thalassaemic patients and malaria. In this research, a series of HPOs with different substitutes and position were theoretically invest

An environmentally friendly, one-pot, three-component synthesis of 8,10-dimethyl-12-aryl-12H-naphtho[1′,2′:5,6]pyrano[2,3-d]pyrimidine-9,11-diones was achieved via coupling aromatic of aldehydes, β-naphthol and 6-amino-1,3-dimethyl uracil in the presence of formic acid as a catalyst under solvent-free conditions at 90 °C. This method has several advantages, such as efficiency, good yield, short...

An expedient synthetic route for 3-aryl beta-carbolin-1-ones was developed starting from ethyl acetamidocyanoacetate and chalcone derivatives. The five- and six-membered nitrogen-containing rings in the beta-carbolin-1-ones were elaborated efficiently by an intramolecular ketone-nitrile annulation and an intramolecular N-arylation of amide respectively.

Synthesis of 4-(N,N- dimethylamino)-3-aryl-3-butene-2-one, ethyl-5-aryl-4-oxo-4H-pyran-2-carboxylate, ethyl-5-aryl-4-pyridones-2-carboxylate and 5-aryl-3-cyano-5-methyl-2-pyridones (aryl=3-thienyl, 2-furyl) are described.