Introduction 1.1

Quinazoline Pharmaceuticals

Quinazoline (1) is 1,3-diazanaphthalene. It is also known as 5,6-benzopyri-midine or benzo[a]pyrimidine, or phenmiazine [1], and its4-oxo derivative is called 4(3H)-quinazolinone (2) [2-4] (Fig. 1). Quinazoline and quinazolinone derivatives have continued to attract a widespread interest for a long time due to their diverse pharmacological activities such as antibacterial [5,6], anti-tubecular [7], antifungal [8], antihyperglysemic [9], anti-inflammatory [10], bronchodilatory [11], cholineesterase inhibitor [12], antifolate [13,14], antitumor [15-17], protein kinase inhibitor [18] and many others [2,17]. A vast number of quinazoline derivatives have been synthesized to provide synthetic drugs and to design more effective medicines. There are a number of reviews [2-4,19-29] and monographs [30-32] on quinazoline and quinazoline alkaloids.

As the actual example, methaqualone (3) [33-35] is perhaps the most well-known synthetic quinazoline drug, which was first synthesized in

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