Jul - Aug 2006 Convenient Synthesis of Some 1057 2 - Substituted 4 ( 3 H ) - Quinazolinone Derivatives

4(3H)-Quinazolinones 1 are known for more than a century [1]. Molecules based on quinazoline and quinazolinone exhibit a multitude of interesting pharmacological activities [2], including anticonvulsant, antibacterial and antidiabetic activity [3,4]. The important natural and synthetic 4(3H)-quinazolinones include l-vasicinone 2 [5], chrysogine 3 [6], methaquinalon 4 [7] – a sedative, piriqualone 5 [8,9] – an anticonvulsant, although the latter type of activity does not seem confined to pyridine derivatives of 4(3H)-quinazolinone [10]. Febrifugine 6 and isofebrifugine 7 were known as potent but toxic antimalarial agents long before their initial isolation [11] and recent chemical studies [12-15].