STEREOSPECIFIC SYNTHESIS PROCESS FOR TRETINOIN COMPOUNDS
    1.
    发明公开
    STEREOSPECIFIC SYNTHESIS PROCESS FOR TRETINOIN COMPOUNDS 有权
    丁二酮化合物的立体异构合成方法

    公开(公告)号:EP2708530A1

    公开(公告)日:2014-03-19

    申请号:EP12786430.4

    申请日:2012-05-07

    IPC分类号: C07C403/20

    摘要: A stereospecific synthesis process for tretinoin compounds comprises the following steps: using substituted triphenyl phosphine salt and β-formyl crotonic acid as raw material to carry out WITTIG reaction under the action of alkali; then adjusting the pH of the reaction liquid to 5-10; adding palladium compound or rhodium compound to carry out isomerization directly and obtain tretinoin compounds with desired configuration. The product yield of the process is high and the intermediate product in the reaction dose not need to be separated. The process is easy to operate and can save the production cost and as well is suitable for industrial production.

    摘要翻译: 一种维甲酸化合物的立体有择合成方法,包括以下步骤:以取代的三苯膦盐和β-甲酰巴豆酸为原料,在碱作用下进行WITTIG反应; 然后将反应液的pH调节至5-10; 直接加入钯化合物或铑化合物进行异构化反应,得到具有所需构型的维甲酸化合物。 该方法的产物收率高并且反应中的中间产物不需要分离。 该工艺操作简单,可以节省生产成本,也适用于工业生产。