A series of novel 4-arylaminoquinazolines based on 2-methylthio-6,7,8-trifluoroquinazolin-4(3 H )-one has been synthesized. It was found that interaction of these compounds with cycloalkylimines leads to the substitution of F7 atom and methylthio group at position 2 retains. 6,7,8-Trifluoro-2-methylthio-4-(2-methoxyphenylamino)quinazoline demonstrated tuberculostatic activity in vitro (MIC 1.5 μg/mL).