申请人:Vass Andras
公开号:US20080039643A1
公开(公告)日:2008-02-14
The invention relates to a process for the preparation of a phenolic hydroxy-substituted compound of the general formula (I) by desalkylation of an alkyl aryl ether of the general formula (II) by treatment with a thiourea/aluminum chloride reagent pair, in said general formulae R
1
stands for straight chain or branched C
1-6
alkyl group; R
2
, R
3
, R
4
, R
5
, and R
6
have the same or different meanings and stand for hydrogen or halogen atom, hydroxy, carboxy, nitro, oxo, C
1-6
alkylcarbonyl, straight chain or branched alkyl or -alkoxy, or aryl group, or R
2
and R
3
together stand for a 5-7 membered ring or fused ring system; said 5-7 membered ring may be a partially saturated ring optionally substituted with an oxo group or can be an unsaturated ring; or said fused ring system may constitute with the first ring a steroid, preferably an estratriene derivative optionally substituted with an oxo or C
1-6
alkylcarbonyloxy group in the 17 position.
本发明涉及一种制备羟基取代酚类化合物的方法,其通式为(I),通过使用硫脲/氯化铝试剂对通式(II)的烷基芳基醚进行脱烷基化处理,其中,通式中R1代表直链或支链C1-6烷基;R2、R3、R4、R5和R6具有相同或不同的含义,代表氢原子或卤素原子、羟基、羧基、硝基、氧代、C1-6烷基羰基、直链或支链烷基或-烷氧基或芳基基团,或R2和R3共同代表一个5-7成员环或融合环系统;所述5-7成员环可以是一个部分饱和的环,可选地取代有一个氧代基,或者可以是一个不饱和的环;或者所述融合环系统可以与第一个环构成一种类固醇,优选为一种17位置可选地取代有氧代或C1-6烷基羰氧基的雌三烯衍生物。