Process for the preparation of phenolic hydroxy-substituted compounds
    9.
    发明授权
    Process for the preparation of phenolic hydroxy-substituted compounds 有权
    酚羟基取代化合物的制备方法

    公开(公告)号:US07973185B2

    公开(公告)日:2011-07-05

    申请号:US11577434

    申请日:2005-12-07

    Abstract: 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 R1 stands for straight chain or branched C1-6 alkyl group; R2, R3 , R4 , R5, and R6 have the same or different meanings and stand for hydrogen or halogen atom, hydroxy, carboxy, nitro, oxo, C1-6 alkylcarbonyl, straight chain or branched alkyl or -alkoxy, or aryl group, or R2 and R3 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 C1-6 alkylcarbonyloxy group in the 17 position.

    Abstract translation: 本发明涉及一种制备通式(I)的酚羟基取代的化合物的方法,该方法通过在所述的硫脲/氯化铝试剂对中用硫脲/氯化铝试剂对进行脱烷基处理来制备通式(Ⅱ)的烷基芳基醚 通式R1代表直链或支链C 1-6烷基; R2,R3,R4,R5和R6具有相同或不同的含义,代表氢或卤素原子,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, 或R 2和R 3一起代表5-7元环或稠环体系; 所述5-7元环可以是任选被氧代基取代的部分饱和的环,或者可以是不饱和环; 或所述稠环体系可以与第一环一起构成类固醇,优选在17位任选被氧代或C 1-6烷基羰基氧基取代的雌三烯衍生物。

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