The synthesis of acyl N-Boc-1- and N-Boc-2-naphthylamines and their transformation into alkyl substituted benzoquinazolines and benzoquinazolinones through the reaction with formamide or potassium cyanate in the presence of ammonium acetate is described. Presented acyl derivatives were obtained from the reactions of the corresponding lithiated N-Boc naphthylamines with various acetylating agents like AcCl, Ac2O, AcOEt, PivCl, iPrCOCl and also Wienreb amides. Biological screening of the potential cytotoxicity on the HT29 cell line and lymphocytes were demonstrated for some benzoquinazoline derivatives.