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    Method for preparing 4-(6-amino-purin-9-YL)-2(S)-hydroxy-butyric acid methyl ester
    3.
    发明授权
    Method for preparing 4-(6-amino-purin-9-YL)-2(S)-hydroxy-butyric acid methyl ester 有权
    制备4-（6-氨基嘌呤-9-YL）-2（S） - 羟基 - 丁酸甲酯的方法

    公开(公告)号：US08247549B2

    公开(公告)日：2012-08-21

    申请号：US12747312

    申请日：2008-11-06

    申请人： Fajun Nan ,  Jianping Zuo ,  Yangming Zhang ,  Min Gu ,  Wei Tang

    发明人： Fajun Nan ,  Jianping Zuo ,  Yangming Zhang ,  Min Gu ,  Wei Tang

    IPC分类号： C07D473/34

    CPC分类号： C07D473/34 ,  Y02P20/55

    摘要： The present invention discloses a novel method for preparing and purifying 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester. The preparation started from cheap and easily available L-malic acid, which was transformed to intermediate I after simultaneous protection of the groups of 1-carboxyl and 2-hydroxyl. The intermediate I was selectively reduced to intermediate alcohol II, whose hydroxyl group was further transformed to an easily leaving group to afford intermediate III. The intermediate III was nucleophilically substituted with adenine to afford intermediate IV. The intermediate IV was deprotected and methyl-esterified simultaneously in methanol in the presence of an acid or a base to afford crude 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester, which was purified by recrystallization to afford the purified product. Comparing with the prior preparation methods, the present method has advantages in low cost, mild conditions, high retention of the chiral center during the reaction, high productivity, great improvement in the quality and yield of the product and great decrease in cost, and thus is suitable for the production on a large scale.

    摘要翻译： 本发明公开了一种制备和纯化4-（6-氨基嘌呤-9-基）-2（S） - 羟基 - 丁酸甲酯的新方法。 该制剂从便宜且易于获得的L-苹果酸开始，其在同时保护1-羧基和2-羟基的基团后转化为中间体I. 将中间体I选择性还原成中间体醇II，其中羟基进一步转化为容易离去的基团，得到中间体III。 中间体III被腺嘌呤亲核取代，得到中间体IV。 将中间体IV在酸或碱的存在下在甲醇中同时脱甲基酯化，得到粗制的4-（6-氨基 - 嘌呤-9-基）-2（S） - 羟基 - 丁酸甲酯， 通过重结晶纯化，得到纯化产物。 与现有的制备方法相比，本发明方法具有成本低，条件温和，反应中手性中心保留性高，生产效率高，产品质量和产量大幅提高，成本大幅降低的优点， 适合大规模生产。

    Water-soluble artemisinin derivatives, their preparation methods, the pharmaceutical compositions and the use thereof
    4.
    发明授权
    Water-soluble artemisinin derivatives, their preparation methods, the pharmaceutical compositions and the use thereof 有权
    水溶性青蒿素衍生物，其制备方法，药物组合物及其用途

    公开(公告)号：US08129426B2

    公开(公告)日：2012-03-06

    申请号：US11989135

    申请日：2006-07-20

    申请人： Ying Li ,  Jianping Zuo ,  Zhongshun Yang ,  Junxia Wang ,  Yu Zhang ,  Wei Tang ,  Jianxin Zhang

    发明人： Ying Li ,  Jianping Zuo ,  Zhongshun Yang ,  Junxia Wang ,  Yu Zhang ,  Wei Tang ,  Jianxin Zhang

    IPC分类号： A61K31/35

    CPC分类号： C07D493/18

    摘要： Water-soluble artemisinin derivatives, their preparation methods, the pharmaceutical compositions containing the same derivatives and the use thereof are disclosed. The artemisinin derivatives have following formula I. It has been proved by pharmacological tests that these compounds and compositions have evident immuno-suppressive activities, and may be used in the preparation of novel immuno-suppressants for treating the diseases caused by hyperfunction of human immunity (e.g. the auto-immune diseases such as lupus erythematosus, rheumatoid arthritis, multiple sclerosis and the like), and for inhibiting the graft rejection after cell or organ transplantation.

    摘要翻译： 公开了水溶性青蒿素衍生物及其制备方法，含有相同衍生物的药物组合物及其用途。 青蒿素衍生物具有以下式I：通过药理学实验证明，这些化合物和组合物具有明显的免疫抑制活性，可用于制备用于治疗由人免疫功能障碍引起的疾病的新型免疫抑制剂（ 例如自身免疫疾病如红斑狼疮，类风湿性关节炎，多发性硬化症等），以及用于抑制细胞或器官移植后的移植排斥反应。

    Method for Preparing 4-[9-(6-Aminopurine)]-2-(S)-Hydroxyl-Butyric Acid Methyl Ester
    7.
    发明申请
    Method for Preparing 4-[9-(6-Aminopurine)]-2-(S)-Hydroxyl-Butyric Acid Methyl Ester 有权
    4- [9-（6-氨基嘌呤）] - 2-（S） - 羟基 - 丁酸甲酯的制备方法

    公开(公告)号：US20110201810A1

    公开(公告)日：2011-08-18

    申请号：US12747312

    申请日：2008-11-06

    申请人： Fajun Nan ,  Jianping Zuo ,  Yangming Zhang ,  Min Gu ,  Wei Tang

    发明人： Fajun Nan ,  Jianping Zuo ,  Yangming Zhang ,  Min Gu ,  Wei Tang

    IPC分类号： C07D473/34

    CPC分类号： C07D473/34 ,  Y02P20/55

    摘要： The present invention discloses a novel method for preparing and purifying 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester. The preparation started from cheap and easily available L-malic acid, which was transformed to intermediate I after simultaneous protection of the groups of 1-carboxyl and 2-hydroxyl. The intermediate I was selectively reduced to intermediate alcohol II, whose hydroxyl group was further transformed to an easily leaving group to afford intermediate III. The intermediate III was nucleophilically substituted with adenine to afford intermediate IV. The intermediate IV was deprotected and methyl-esterified simultaneously in methanol in the presence of an acid or a base to afford crude 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester, which was purified by recrystallization to afford the purified product. Comparing with the prior preparation methods, the present method has advantages in low cost, mild conditions, high retention of the chiral center during the reaction, high productivity, great improvement in the quality and yield of the product and great decrease in cost, and thus is suitable for the production on a large scale.

    摘要翻译： 本发明公开了一种制备和纯化4-（6-氨基嘌呤-9-基）-2（S） - 羟基 - 丁酸甲酯的新方法。 该制剂从便宜且易于获得的L-苹果酸开始，其在同时保护1-羧基和2-羟基的基团后转化为中间体I. 将中间体I选择性还原成中间体醇II，其中羟基进一步转化为容易离去的基团，得到中间体III。 中间体III用腺嘌呤亲核取代，得到中间体IV。 将中间体IV在酸或碱的存在下在甲醇中同时脱甲基酯化，得到粗制的4-（6-氨基 - 嘌呤-9-基）-2（S） - 羟基 - 丁酸甲酯， 通过重结晶纯化，得到纯化产物。 与现有的制备方法相比，本发明方法具有成本低，条件温和，反应中手性中心保留性高，生产效率高，产品质量和产量大幅提高，成本大幅降低的优点， 适合大规模生产。

    Water-Soluble Artemisinin Derivatives, Their Preparation Methods, the Pharmaceutical Compositions and the Use Thereof
    9.
    发明申请
    Water-Soluble Artemisinin Derivatives, Their Preparation Methods, the Pharmaceutical Compositions and the Use Thereof 有权
    水溶性青蒿素衍生物及其制备方法，药物组合物及其用途

    公开(公告)号：US20090298881A1

    公开(公告)日：2009-12-03

    申请号：US11989135

    申请日：2006-07-20

    申请人： Ying Li ,  Jianping Zuo ,  Zhongshun Yang ,  Junxia Wang ,  Yu Zhang ,  Wei Tang ,  Jianxin Zhang

    发明人： Ying Li ,  Jianping Zuo ,  Zhongshun Yang ,  Junxia Wang ,  Yu Zhang ,  Wei Tang ,  Jianxin Zhang

    IPC分类号： A61K31/357 ,  C07D493/14 ,  A61K31/4025 ,  A61K31/453

    CPC分类号： C07D493/18

    摘要： Water-soluble artemisinin derivatives, their preparation methods, the pharmaceutical compositions containing the same derivatives and the use thereof are disclosed. The artemisinin derivatives have following formula I. It has been proved by pharmacological tests that these compounds and compositions have evident immuno-suppressive activities, and may be used in the preparation of novel immuno-suppressants for treating the diseases caused by hyperfunction of human immunity (e.g. the auto-immune diseases such as lupus erythematosus, rheumatoid arthritis, multiple sclerosis and the like), and for inhibiting the graft rejection after cell or organ transplantation.

    摘要翻译： 公开了水溶性青蒿素衍生物及其制备方法，含有相同衍生物的药物组合物及其用途。 青蒿素衍生物具有以下式I：通过药理学实验证明，这些化合物和组合物具有明显的免疫抑制活性，可用于制备用于治疗由人免疫功能障碍引起的疾病的新型免疫抑制剂（ 例如自身免疫疾病如红斑狼疮，类风湿性关节炎，多发性硬化症等），以及用于抑制细胞或器官移植后的移植排斥反应。