Microwave-assisted one-pot synthesis of 2,3-disubstituted 3H-quinazolin-4-ones

Review of Microwave-Assisted Synthesis of Benzo-Fused Six-MemberedN,N-Heterocycles

“…It is noteworthy that this condensation furnished a much lower yield of 60% in a considerably longer reaction time of 5-8 h when carried out under conventional heating conditions at a maximum temperature of 120 o C (Schemes 34 and 35). [97][98] An interesting investigation regarding the microwave-assisted synthesis of biologically potent alkaloids has recently been reported by J.-F. Liu et al [99] The authors initially explored a microwave-assisted one-pot synthesis of the 2,3-disubstituted 3H-quinazolin-4-one skeleton, a privileged structure present in many biologically interesting alkaloids such as the sedativehypnotic Methaqualone, antitussive Chloroqualone and anticonvulsant Piriqualone. [100][101][102] The quinazolinone core is found in a variety of natural products possessing interesting bioactivity, such as anti-inflammatory, cardiovascular, CNS, antimalarial and antiviral effects.…”

Microwave-Assisted Natural Product Chemistry

“…An interesting investigation regarding the microwave-assisted synthesis of biologically potent alkaloids has recently been reported by J.-F. Liu et al [78]. The authors initially explored a microwave-assisted one-pot synthesis of the 2,3-disubstituted 3H-quinazolin-4-one skeleton, a privileged structure present in many biologically interesting alkaloids such as the sedativehypnotic Methaqualone, antitussive Chloroqualone and anticonvulsant Piriqualone [79][80][81].…”

Synthesis of a series of carbon‐14 labelled 4‐aminoquinazolines and quinazolin‐4 (3H)‐ones

“…In both cases however, to ensure optimum yield of products, an excess of formic acid 8 had to be employed. [14][15][16] On the other hand, using the known Niementowski reaction, 17,18 the condensation of formamide 9 with 6a under microwave irradiation, gave the desired product 2 in a few minutes.…”