Синтез и биологические свойства производных 5-метил-5-этил-4-оксобензо[h]хиназолинов

9-Methyl-9-ethyl-8-oxo-2,3,4,5,6,7,9,10-octahydrobenzo[h]azepino[2,1-b]quinazoline was obtained via interaction between 1-amino-3-methyl-3-ethyl-2-ethoxycarbonyl-3,4-dihydronaphthalene (aminoester) and caprolactam in the presence of phosphorus oxychloride. 5-Methyl-5-ethyl-4-oxo-3,4,5,6-tetrahydrobenzo[h]quinazoline was synthesized using the reaction of aminoester with formamide under the conditions of Niementowski reaction. This aminoester reacts with benzoylisothiocyanate at room temperature with the formation of N-benzoylthiureidoderivative, which exhibits cyclization in the presence of an alkali, yielding 5-methyl-5-ethyl-4-oxo-2-thioxo-l,2,3,4,5,6-hexahydrobenzo[h]quinazoline. The latter is converted into 2-substituted-5-methyl-5-ethyl-4-oxo-3,4,5,6-tetrahydrobenzo[h]quinazolines by reactions with alcyl-, allyl-, benzylhalogenides, 2-bromethanol, ester and amides of halogen-substituted acetic acids. The effect of compounds on monoaminooxidase (MAO) activity in vitro and in vivo and antitumour properties of some compounds were studied. It is established that synthesized compounds possess antitumour and anti-MAO properties.