ChemInform Abstract: Synthesis of 2,3‐Disubstituted Quinazolin‐4(3H)‐ones

Efficient and Practical One-Pot Route to Synthesise Quinazolin4(3H)-Ones Using Trifluoromethanesulfonic Anhydride and 2-Chloropyridine

“…Melting points were taken on a Kofler hot stage apparatus and are uncorrected. 1 H and 13 C NMR spectra were recorded on a Bruker FT-500 instrument, using TMS as an internal standard. Elemental analysis was performed with an Elementar Analysensystem GmbH VarioEL CHNS mode.…”

“…Quinazolinone derivatives are essential units in a wide range of relevant pharmacophores with a broad spectrum of abilities. 1 Due to their wide range of pharmacological and therapeutic activities including anticonvulsant, 2 anti-inflammatory, 3 hypolipidemic, 4 anticancer 5 and anti-ulcer, 6 the synthesis of quinazolinone moieties as a privileged class of fused heterocyclic compounds 7 has attracted researchers' attention. In recent years, several synthetic routes have been introduced for the preparation of 4(3H)-quinazolinone derivatives in which the condensation of a 2-aminobenzoic acid or its derivatives with amides has been mentioned as the most common synthetic approach.…”

Multicomponent reaction of benzyl halides: Synthesis of [1,2,4]triazolo/benzimidazolo quinazolinones

“…[20] Hence, the synthesis of quinazolinone has evoked much interest, as a result of which a variety of synthetic methodologies have been reported. [21][22][23] The most important approaches are (i) one-pot condensation of aromatic aldehydes, 2-amino benzimidazole/3-amino-1,2,4-triazole, and α-hydroxy C-H acids, [24] (ii) three-component reaction of 2-amino benzamides, aryl halides, and isocyanides, [25] (iii) one-pot reaction with o-amino benzamides and primary alcohols, [26] (iv) cascade synthesis of phenylamino substituted quinazolinones from urea derivatives and tert-butyl isocyanide, [27] [v] oxidative radical skeletal rearrangement induced by oxygen, [28] (vi) synthesis of quinazolinone and quinazoline from aerobic oxidative C(sp3)À H amination/ CÀ N cleavage. [29] Other methods have also been developed within the past three decades.…”

CuBr/Et3N‐Promoted Reactions of 2‐Aminobenzamides and Isothiocyanates: Efficient Synthesis of Novel Quinazolin‐4(3H)‐ones

“…At this juncture, medicinal properties, such as antiulcer , anticancer , anti‐inflammatory , anticonvulsant , hypolipidemic , antifungal , antiviral , and anti‐coccidial , have been the center of attention for medicinal chemists. Therefore, several procedures have been reported for the synthesis of quinazolin‐4(3 H )‐ones .…”