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    • 4. 发明申请
    • METHOD FOR PRODUCING STEROID COMPOUND
    • 生产甾体化合物的方法
    • US20100063272A1
    • 2010-03-11
    • US12160338
    • 2007-01-12
    • Jun TakeharaNaoya FujiwaraKyouko EndouJunya KawaiAkemi HosokawaNaoko Sumitani
    • Jun TakeharaNaoya FujiwaraKyouko EndouJunya KawaiAkemi HosokawaNaoko Sumitani
    • C07J71/00C07J9/00C07C29/10
    • C07J9/005C07J17/00
    • It is an object of the present invention to provide a novel method for producing a steroid compound. The present invention provides a method for producing 5β-3,7-dioxocholanic acid or an ester derivative thereof, using, as a raw material, a sterol having double bonds at position 5 and at position 24, such as cholesta-5,7,24-trien-3β-ol, ergosta-5,7,24(28)-trien-3β-ol, desmosterol, fucosterol, or ergosta-5,24(28)-dien-3β-ol, via the following 4 steps:(I) a step involving oxidation of a hydroxyl group at position 3 and isomerization of a double bond at position 5 to position 4; (II) a step involving the oxidative cleavage of a side chain to convert position 24 to a carboxyl group or an ester derivative thereof; (III) a step of introducing an oxygen functional group into position 7; and (IV) a step of constructing a 5β configuration by reductive saturation of a double bond at position 4.
    • 本发明的目的是提供一种制备类固醇化合物的新方法。 本发明提供了使用在5位和24位具有双键的甾醇如胆石酯-5,7制备作为原料的5αb-三 - (3,7-二氧代胆烷酸)或其酯衍生物的方法 ,24-三烯-3β-醇,麦角甾-5,7,24(28) - 三烯-3β-醇,去极化醇,岩藻甾醇或麦角甾-5,24(28) - 二烯-3β-醇, 以下4个步骤:(I)涉及氧化位置3处的羟基并将位置5的双键异构化到位置4的步骤; (II)涉及侧链的氧化断裂以将位置24转化为羧基或其酯衍生物的步骤; (III)将氧官能团引入位置7的步骤; 和(四)构建5&bgr的步骤; 通过在位置4的双键的还原饱和构型。