세사몰 유도체 또는 그의 염, 그의 제조방법, 및 이를함유하는 피부외용제 조성물
    71.
    发明公开
    세사몰 유도체 또는 그의 염, 그의 제조방법, 및 이를함유하는 피부외용제 조성물 有权
    SESAMOL衍生物或其盐,其制备方法和含有其的皮肤外用组合物

    公开(公告)号:KR1020060130835A

    公开(公告)日:2006-12-20

    申请号:KR1020050048717

    申请日:2005-06-08

    CPC classification number: A61K8/55 A61K2800/522 A61Q19/08 C07F9/65517

    Abstract: Sesamol derivatives or their salts, a process for preparing the same compounds, and a skin external composition containing the same compounds are provided to prevent aging of the biological membrane by slowly releasing sesamol and 3-aminopropan phosphate, and reduce the skin irritation. The sesamol derivatives represented by the formula(I) or their salts are provided, wherein the salt is alkali metal salt or alkali earth metal salt. The process for preparing the sesamol derivatives represented by the formula(I) or their salts comprises the steps of: (A) reacting sesamol with phosphorus oxychloride in the presence of organic base at 12-18 deg. C for 1-2 hours to prepare dichloro[3,4-methylene dioxy penoxy]-phosphino-1-one; (B) reacting the dichloro[3,4-methylene dioxy penoxy]-phosphino-1-one with organic solvent in the presence of base to prepare [3,4-methylene dioxy penoxy]-1,3,2-oxazaphosphorin P-oxide; (C) after filtering the reaction solution and concentrating the filtered solution under reduced pressure, adding the acid solution into the concentrate and reacting them at 5-100 deg. C for 3-12 hours to prepare sesamol(3-aminopropane phosphate diester); and (D) crystallizing the sesamol(3-aminopropane phosphate diester) by slowly dropping polar organic solvent into the sesamol.

    Abstract translation: 提供芝麻酚衍生物或其盐,制备相同化合物的方法和含有相同化合物的皮肤外用组合物,以通过缓慢释放芝麻酚和3-氨基丙酸磷酸盐来防止生物膜的老化,并减少皮肤刺激。 提供由式(I)表示的芝麻酚衍生物或其盐,其中盐为碱金属盐或碱土金属盐。 制备由式(I)表示的芝麻酚衍生物或其盐的方法包括以下步骤:(A)在有机碱的存在下在12-18℃使芝麻酚与磷酰氯反应。 C 1-2小时制备二氯[3,4-亚甲二氧二氧基] - 膦酰基-1-酮; (B)在碱存在下使二氯[3,4-亚甲二氧基二氧基]膦基-1-酮与有机溶剂反应,制备[3,4-亚甲基二氧基壬氧基] -1,3,2-氧杂磷杂环磷酸P- 氧化物; (C)过滤反应溶液后,减压浓缩滤液,加入酸溶液至浓缩物,并在5〜100℃反应。 3〜12小时制备芝麻酚(3-氨基丙烷磷酸二酯); 和(D)通过将极性有机溶剂缓慢滴入芝麻酚中来结晶芝麻酚(3-氨基丙烷磷酸二酯)。

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