Approach for synthesis of catechins
    7.
    发明授权
    Approach for synthesis of catechins 有权
    儿茶素合成方法

    公开(公告)号:US09556140B2

    公开(公告)日:2017-01-31

    申请号:US14763018

    申请日:2014-01-27

    摘要: A process for synthesis of enatiomerically pure or enatiomerically enriched or racemic mixture of (+ and/or −) epicatechin and its intermediates, comprising the steps of: (i) obtaining penta-protected quercetin; (ii) reducing the penta-protected quercetin obtained from step (i); (iii) optionally deprotecting the compound of step (ii); (iv) reducing the compound obtained from step (ii) or step (iii) in the presence of a chiral/achiral reducing agent to obtain a chiral intermediate; (v) deprotecting and/or hydrogenation of the chiral intermediate obtained from step (iv) to obtain (−)-epicatechin; (vi) optionally simultaneously deprotecting and by drogenation of the compound obtained from step (ii) to obtain racemic epicatechin.

    摘要翻译: (+和/或 - )表儿茶素及其中间体的对映体纯的或对映体富集或外消旋混合物的方法,包括以下步骤:(i)获得五保护的槲皮素; (ii)还原由步骤(i)获得的五保护的槲皮素; (iii)任选地使步骤(ii)的化合物脱保护; (iv)在手性/非手性还原剂存在下还原由步骤(ii)或步骤(iii)获得的化合物,得到手性中间体; (v)从步骤(iv)获得的手性中间体的脱保护和/或氢化得到( - ) - 表儿茶素; (vi)任选地同时去除由步骤(ⅱ)获得的化合物脱保护和脱氢,得到外消旋表儿茶素。

    UTILITY OF (+) EPICATECHIN AND THEIR ANALOGS

    公开(公告)号:US20190247359A1

    公开(公告)日:2019-08-15

    申请号:US16311422

    申请日:2017-06-21

    摘要: The present invention pertains to the enhanced activity of (+) epicatechin over (−) epicatechin. The present invention is related to novel analogs of (+) epicatechin of the formula (I), which enhances the pharmacokinetics and therefore the pharmacodynamics of (+) epicatechin. The present invention is related to analogs of (+) epicatechin of the formula (I). The general structure of the analogs of the present invention may be represented by Formula (I): Formula (I) wherein A and B are independently OR1 and C and D are independently OH; wherein R1 is independently C1 to C10 lower straight or branched chain acyclic or cyclic alkyl, or is selected from the group comprising, hydroxy butyric acid, dichloroacetic acid; phenyl butyric acid; valproic acid.