Studies on biologically active halogenated compounds. II. Chemical modifications of 6-amino-2-fluoromethyl-3-(o-tolyl)-4(3H)-quinazolinone and the CNS depressant activities of related compounds.

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Abstract
A number of derivatives of 6-amino-2-fluoromethyl-3-(o-tolyl)-4(3H)-quinazolinone (15), a potent muscle relaxant, were prepared and screened in terms of the loss of righting reflex test and the rotating rod test in mice. Several derivatives with additional Fl substitution or with repositioning of the Fl atom exhibited high activities. Other structural modifications included acylation, carbamoylation and alkoxycarbonylation of the 6-amino group, hydroxylation at the 3-tolyl group and replacement of the Fl atom at the 2-fluoromethyl group by O2, N and S nucleophiles; these modifications caused loss of activity.

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