Method for producing antifolate agents having glutamic acid part in their structure
    1.
    发明授权
    Method for producing antifolate agents having glutamic acid part in their structure 有权
    在其结构中制备具有谷氨酸部分的抗叶酸剂的方法

    公开(公告)号:US08680319B2

    公开(公告)日:2014-03-25

    申请号:US13990770

    申请日:2010-12-03

    IPC分类号: C07C303/00

    CPC分类号: C07D475/08 C07C51/08

    摘要: A method for producing antifolate agents having glutamic acid part in their structure is developed by protecting carboxyl groups of glutamic acid or its N-substituted derivatives as cyanomethyl ester to give compounds of formula (II) which are hydrolyzed under very mild conditions to afford antifolate agents in high yield with high analytical and optical purity.

    摘要翻译: 通过保护谷氨酸的羧基或其N-取代的衍生物作为氰甲基酯来制备具有其结构中具有谷氨酸部分的抗叶酸剂的方法,得到在非常温和的条件下水解的式(II)化合物以提供抗叶酸剂 高产率,高分析和光学纯度。

    Method for producing antifolate agents having glutamic acid part in their structure
    2.
    发明申请
    Method for producing antifolate agents having glutamic acid part in their structure 有权
    在其结构中制备具有谷氨酸部分的抗叶酸剂的方法

    公开(公告)号:US20130253192A1

    公开(公告)日:2013-09-26

    申请号:US13990770

    申请日:2010-12-03

    IPC分类号: C07D475/08 C07C51/08

    CPC分类号: C07D475/08 C07C51/08

    摘要: A new method for producing antifolate agents having glutamic acid part in their structure is developed by protecting carboxyl groups of glutamic acid or its N-subsituted derivatives as cyanomethyl ester to give compounds of formula (II) which are hydrolyzed under very mild conditions to afford antifolate agents in high yield with high analytical and optical purity.

    摘要翻译: 通过保护谷氨酸或其N-取代的衍生物的羧基作为氰甲基酯来制备具有其结构中具有谷氨酸部分的抗叶酸剂的新方法,得到在非常温和的条件下水解以得到抗叶酸剂的式(II)化合物 高产率的高分子和光学纯度的试剂。

    Process for the preparation of 4-amino-1-hydroxybutylidene-1, 1-biphosphonic acid
    4.
    发明授权
    Process for the preparation of 4-amino-1-hydroxybutylidene-1, 1-biphosphonic acid 失效
    制备4-氨基-1-羟基亚丁基-1,1-双膦酸的方法

    公开(公告)号:US07009071B2

    公开(公告)日:2006-03-07

    申请号:US10473600

    申请日:2002-05-08

    IPC分类号: C07C229/01 C07C225/163

    CPC分类号: C07F9/3873

    摘要: This invention is related with the preparation of 4-amino-1-hydroxybutylidene-1,1-biphosphonic acid or salts thereof. The reaction of 4-aminobutyric acid with phosphorous acid and phosphorus trichloride in the presence of aralkyl or alkyl ethoxylates or triglycerides such as plant or animal oils or their derivatives; and recovering of 4-amino-1-hydroxybutylidene-1,1-biphosphonic acid or salts thereof are described. The main feature of the invention is in the use of the above defined non-ionic emulgators in the phosphonylation reaction.

    摘要翻译: 本发明涉及4-氨基-1-羟基亚丁基-1,1-二膦酸或其盐的制备。 在芳烷基或烷基乙氧基化物或甘油三酸酯如植物或动物油或其衍生物存在下,4-氨基丁酸与亚磷酸和三氯化磷的反应; 并描述了4-氨基-1-羟基亚丁基-1,1-二膦酸或其盐的回收。 本发明的主要特征是在膦酰化反应中使用上述定义的非离子乳化剂。