A novel and efficient route for the preparation of quinazolin-4(3H)-imines via a palladium-catalyzed three-component reaction of carbodiimide, isocyanide, and nucleophile is described. The palladium-catalyzed isocyanide insertion is believed to be the key step during the reaction process.

The title mol-ecule, C12H11Cl3N2O2, contains planar quinazolin-4(3H)-one (r.m.s. deviation = 0.0257 Å) and propyl fragments, forming a dihedral angle of 10.4 (2)°. An intra-molecular O-H⋯N hydorgen bond occurs. In the crystal, O-H⋯O hydrogen bonds link the mol-ecules into an infinite chain running parallel to the b axis.

An interesting procedure for the synthesis of isoindolo[1,2-b]quinazolin-10(12H)-ones has been developed. Starting from commercially available 2-bromoanilines and 2-bromobenzyl amines, with the assistance of a palladium catalyst, the desired products were isolated in good yields. Notably, this procedure proceeded in a highly selective manner; two molecules of CO were incorporated into the subst...

We herein describe the rapid synthesis of a diverse set of dihydroquinazolin-4-ones and quinazolin-4-ones, their biological evaluation as thyroid stimulating hormone receptor (TSHR) agonists, and SAR analysis. Among the compounds screened, 8b was 60-fold more potent than the hit compound 1a, which was identified from a high throughput screen of over 73,000 compounds.

Herein we describe the synthesis and evaluation of a series of novel 2,3-dihydro-1H-pyrrolo[3,2,1-ij]quinazolin-1-ones for in vitro cytotoxicity against three human cancer cell lines as well as for potential antimalarial activity against the chloroquine-sensitive strain 3D7 of Plasmodium falciparum. The title compounds were prepared via PdCl₂-mediated endo-dig cyclization of 2-aryl-8-(arylethyn...

In this work, it was of interest to synthesize new series of some 2-[(E)-2-furan-2-yl-vinyl]-quinazolin-4(3H)-ones incorporated into pyrazoline, isoxazoline, pyrimidine or pyrimidine-thione ring systems at position-3 of the quinazoline ring. The antimicrobial activity and antiinflammatory effect of some of these compounds were studied.

1,1-Disubstituted-3-(2-phenyl-3H-quinazolin-4-ylidene)thioureas (8) were synthesized in a one pot reaction of N-(2-cyanophenyl)benzimidoyl isothicyanate (3) with secondary amines. The products underwent transamination reactions. Compounds 8a-8g were identified by FTIR, H-NMR, C-NMR, mass spectroscopy and X-ray crystallography.

Quinazolines exhibit various biological activities. In the present investigation a series of new 2-amino-5-aryl5,6-dihydro7-(naphthalen-2-yl)quinazolin-4-ols are synthesized by the condensation of various naphthyl substituted cyclohexenones with guanidine in presence of NaOEt. All the synthesized compounds are characterized by various spectral techniques.

The title compound, C(15)H(16)N(2)O(2)·H(2)O, was synthesized via the alkyl-ation of 3-hydroxy-methyl-idene-2,3-dihydro-1H-pyrrolo[2,1-b]quinazolin-9-one with n-propyl iodide in the presence of sodium hydroxide. The organic mol-ecule and the water mol-ecule both lie on a crystallographic mirror plane. In the crystal structure, inter-molecular O-H⋯O and O-H⋯N hydrogen bonds link the components i...