The title mol-ecule, C(22)H(17)BrN(2)O(4)S, has a twisted U shape, the dihedral angle between the quinazolin-4-one and bromo-benzene ring systems being 46.25 (8)°. In order to avoid steric clashes with adjacent substituents on the quinazolin-4-one ring, the N-bound tolyl group occupies an orthogonal position [dihedral angle = 89.59 (8)°]. In the crystal, mol-ecules are connected into a three-di...

The hitherto unknown bis[quinazolin-4-one-2-yl]-m-phenylene (2d), and its 3-N-substituted derivatives were prepared from the corresponding bis[3,1-benzoxazin-4-one-2-yl]-m-phenylene (1) as precursor. The quinazolinone derivative 2d was converted into bis[quinazolin-4-thioxo-2-yl]-m-phenylene (3) via different routes, bis[4-chloroquinazolin-2-yl]-m-phenylene (8) and bis[4-hydrazinoquinazolin-2-y...

Aryltellurium trichlorides have proven themselves as good cyclizing reagents in electrophilic intramolecular cyclization reactions, mainly of propenyl derivatives heterocycles. On the other hand, information on use butenyl reactions with p-alkoxyphenyltellurtrichlorides is limited. In this work, regioselectivity process but-2-enyl thioethers quinoline-3carbaldehyde and quinazolin-4-one p-methox...

2-(1-(4-Bromophenyl)-2-thiocyanatoethylidene)malononitrile (3) undergoes azo coupling with diazotized aromatic amines to afford arylhydrazone derivatives, which are readily cyclized to afford the corresponding 3(2H)-pyridazinimine derivatives upon reflux in aqueous NaOH. Under similar condition an o-cyanoarylhydrazone derivative was cyclized into 6H-pyridazino[1,6-a]quinazolin-6-imine, which in...

A series of novel 2-methyl-3-substituted quinazolin-4-(3H)-ones have been synthesized by treating (2-methyl-4-oxo-3H-quinazolin-3-yl)dithiocarbamic acid methyl ester with different amines, the starting material dithiocarbamate was synthesized from anthranilic acid. The compounds synthesized were investigated for analgesic, anti-inflammatory and antibacterial activities. All the test compounds e...

The metabolism and pharmacokinetics of gefitinib (Iressa®, N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholino-propoxy)quinazolin-4-amine), a selective thymidylate kinase inhibitor for the epider...

Indolo[2,1-b]quinazolin-6,12-dione (tryptanthrin) derivatives present important types of nitrogen-containing heterocyclic compounds which are useful intermediate products in organic synthesis and have potential pharmaceutical applications. The new ethyl 5-oxo-5-(((12-oxoindolo[2,1-b]quinazolin-6(12H)-ylidene)amino)oxy)pentanoate (Compound 2) was synthesized. Compound 2 is the first example a tr...

Vasicine (VAS), a potential natural cholinesterase inhibitor, exhibited promising anticholinesterase activity in preclinical models and has been in development for treatment of Alzheimer's disease. This study systematically investigated the in vitro and in vivo metabolism of VAS in rat using ultra performance liquid chromatography combined with electrospray ionization quadrupole time-of-flight ...

Dimethylformamide dimethylacetal (DMFDMA) is widely used as a source of electrophilic one-carbon units at the formate oxidation level; however, electrophilic methylation with this reagent is previously unreported. Reaction of anthranilamide with DMFDMA at 150 °C for short periods gives mainly quinazolin-4-one. However, prolonged reaction with dimethylformamide di(primary-alkyl)acetals leads to ...

A series of 3-Amantadinyl-2-[(4-amino-3-aryl-5-ylthio)-1,2,4-triazolo]methyl)quinazolin-4-one 5(a-i) were prepared by the reaction of 3-Amantadinyl-2-[(4-acetamido-3-aryl-5-ylthio)-1,2,4-triazolo]methyl)quinazolin-4-one 4(a-i) with various 3-aryl-4-acetamido-5-mercapto triazoles. The compounds 5(a-i) biologically evaluated for their antiinflammatory and antibacterial activities.Structures of th...