发明名称 Hexa:hydro-4-hydroxy-di:benzofuran derivs. - useful as intermediates for analgesic 4-amino cpds.
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>
申请公布号 FR2482966(A1) 申请公布日期 1981.11.27
申请号 FR19800011579 申请日期 1980.05.23
申请人 MAUVERNAY CTRE EUROPEEN RECHERC 发明人 NORBERT BUSCH, MICHEL COMBOURIEU ET JEAN-CLAUDE LAIGLE;COMBOURIEU MICHEL;LAIGLE JEAN-CLAUDE
分类号 C07D307/91;(IPC1-7):07D307/91;61K31/34 主分类号 C07D307/91
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