Process for preparing guggulsterones
    10.
    发明授权
    Process for preparing guggulsterones 有权
    制备苦瓜酮的方法

    公开(公告)号:US07365218B2

    公开(公告)日:2008-04-29

    申请号:US10393408

    申请日:2003-03-20

    IPC分类号: C07J7/10 C07J13/00 C07J1/00

    摘要: The present invention provides an improved process for the preparation of Guggulsterones which comprises epoxidising 16-dihydropegnenolone acetate (16 DPA) by reacting 16DPA with hydrogen peroxide reagent adduct in the presence of a co-base in a polar solvent to obtain 3 β hydroxy-16 α, 17-oxido-5 pregnen-20-one, converting the 3 β hydroxy-16α, 17-oxido-5-pregnen-20-one by reacting with hydrazine in the presence of a strong base at refluxing temperature followed by oxidation to obtain desired guggulsterones viz. to 5, 17-(20)-cis and trans pregnadiene-3 β, 16-diol of the formula Ia and Ib.

    摘要翻译: 本发明提供了一种制备吉格斯酮的改进方法,其包括通过在极性溶剂中在共碱存在下使16DPA与过氧化氢试剂加合物反应,得到3β羟基-16(16DPA),从而使16-二氢异麦角酮酮乙酸酯(16DPA) α,17-氧化-5孕妇-20-酮,通过在强碱存在下在回流温度下与肼反应,将3β羟基-16α,17-氧化-5-孕烯-20-酮转化为氧化至 获得所需的苦瓜子 至5,17-(20) - 顺式和反式孕二烯-3β,16-二醇。