摘要 |
<p>Dibenzofuran derivs. of formula (I) are new: (R1, R2, R3 and R4 are each H, halo, lower alkyl or alkoxy, or trifluoromethyl). (I) are pref. prepd. by yielding an opt. substd. 2-(cyclohexen-2-yl) phenol (II) in a single stage with an organic peracid. Pref. the acid is m-chloroperbenzoic (III) and is added in small portions to a soln. of (II) in e.g. CH2Cl2 at 0 deg.C. The mixt. is then stirred at room temp. for about 4 hr. Pref., the phenolic gp. in (II) is protected by reaction with acetyl chloride, then the prod. reacted with (III) to give an epoxide which is cyclised with alcoholic alkali alkoxide. (I) are converted to 4-amino derivs. (a) by oxidn. to ketone then reaction with amine, or (b) reaction with hydroxylamine then redn. of the oxime formed.</p> |