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    Preparation of 5-aminosalicylic acid by gas phase catalytic carboxylation
    3.
    发明授权
    Preparation of 5-aminosalicylic acid by gas phase catalytic carboxylation 有权
    通过气相催化羧化制备5-氨基水杨酸

    公开(公告)号：US09067867B2

    公开(公告)日：2015-06-30

    申请号：US13997303

    申请日：2011-10-20

    申请人： Guangxing Li ,  Jinjin Li ,  Dajian Zhu ,  Qiang Jiang ,  Lingli Cai ,  Yong Xie ,  Lixin Gan

    发明人： Guangxing Li ,  Jinjin Li ,  Dajian Zhu ,  Qiang Jiang ,  Lingli Cai ,  Yong Xie ,  Lixin Gan

    IPC分类号： C07C229/64 ,  C07C227/18 ,  C07C227/20 ,  C07C231/12

    CPC分类号： C07C229/64 ,  C07C227/20 ,  C07C231/12 ,  C07C233/54

    摘要： Disclosed is a process for preparing 5-aminosalicylic acid by gas phase catalytic carboxylation, characterized in that carbon dioxide is introduced into a system of p-acetaminophenol and a basic compound at a temperature of 150° C.˜220° C. and a pressure of 0.5˜5.0 MPa in the presence of a catalyst, so as to carry out a gas phase catalytic carboxylation reaction to form a 5-aminosalicylate, and the crude product 5-aminosalicylate is separated, and then acidified to prepare 5-aminosalicylic acid (5-ASA). Since the gas phase catalytic reaction replaces a solid phase thermo-chemical reaction, the reaction is significantly improved in terms of the process flow, reaction conditions, product quality and energy consumption. In addition, the reaction has a short reaction time, good selectivity, high yield and no formation of wastes during the reaction, and is suitable for industrial production.

    摘要翻译： 公开了一种通过气相催化羧化制备5-氨基水杨酸的方法，其特征在于在150℃〜220℃的温度下将二氧化碳引入对乙酰氨基苯酚和碱性化合物的体系中， 在催化剂存在下为0.5〜5.0MPa，进行气相催化羧化反应以形成5-氨基水杨酸酯，分离出粗产物5-氨基水杨酸酯，然后酸化以制备5-氨基水杨酸（ 5-ASA）。 由于气相催化反应代替了固相热化学反应，反应在工艺流程，反应条件，产品质量和能耗方面都得到了显着改善。 此外，反应时间短，选择性好，产率高，反应时不产生废物，适用于工业生产。

    Processes for preparing pharmaceutical grade melphalans from industrial grade reactants
    7.
    发明申请
    Processes for preparing pharmaceutical grade melphalans from industrial grade reactants 失效
    从工业级反应物制备药用级别梅毒的方法

    公开(公告)号：US20120190887A1

    公开(公告)日：2012-07-26

    申请号：US12379475

    申请日：2009-02-23

    申请人： Chen Zhou

    发明人： Chen Zhou

    IPC分类号： C07C227/40

    CPC分类号： C07C227/20 ,  C07C229/42

    摘要： A four stage inexpensive method of preparing pharmaceutical grade Melphalans of Melphalan 2-HCl, Melphalan HCl and Melphalan by:reacting N- phthaloyl-4-[bis(2-hydroxyethyl)amino]-phenylalanine ethyl ester with phosphorous oxychloride, reacting the chlorinated product with HCl and alkali hydroxide and purifying, and lyophilizing to obtain Melphalans.

    摘要翻译： 通过以下方法制备美法仑2-HCl，美法仑盐酸盐和美法仑药物级梅尔法兰的四阶段廉价方法：将N-邻苯二甲酰基-4- [双（2-羟乙基）氨基] - 苯基丙氨酸乙酯与磷酰氯反应，使氯化产物 用HCl和碱性氢氧化物进行纯化，并冻干得到Melphalans。