2-Benzazepines. 7. Synthesis of pyrimido[5,4-d][2]benzazepines

Two novel syntheses of pyrimido5,4-d]2]benzazepines are described. The first synthesis started with 3-phenylphthalide which in three steps was converted to a functionalized pyrimidine which was cyclized to give the 2-benzazepine ring system. The second approach used o-benzoylbenzoic acid methyl ester as the starting material, which in four steps was converted to a functionalized pyrimidine which was cyclized to give a 2-benzazepine. Pyrimido5,4-d]2]benzazepines have been found to have activity in standard central nervous system (CNS) pharmacological tests.