Interest in the medicinal chemistry of quinazoline derivatives was stimulated in the early 1950's by the elucidation of the structure of febrifugine (Formula 1), the active principle of the ancient antimalarial preparation eh' ang Shan. 75 Few other quinazoline alkaloids are known,68 but many synthetic derivatives of quinazoline are now available and some display interesting pharmacological properties. Armarego 8 has comprehensively reviewed the general chemistry and pharmacology of quinazoline derivatives.Oxoquinazolines with the general formula (Formula 2) are conveniently obtained by acid-catalyzed condensation of N-acylanthranilic acids with aliphatic or aromatic primary amines or by thermal cycIization of o-aminobenzamides. Methaqualonet itself (Formula 2, R = methyl, R' = 2'-methyl) was first prepared by Kacker and