Process for the preparation of octahydropenta(b)pyrrole carboxylates
    1.
    发明授权
    Process for the preparation of octahydropenta(b)pyrrole carboxylates 失效
    制备甲氧基苯甲酸的方法(B)羧甲基纤维素

    公开(公告)号:US5055591A

    公开(公告)日:1991-10-08

    申请号:US173024

    申请日:1988-03-23

    CPC分类号: C07K5/0222 A61K38/00

    摘要: The invention relates to a process for the preparation of compounds of the formula I ##STR1## in which n is 1 or 2, R denotes hydrogen or an organic radical, R.sup.1 denotes an organic radical, R.sup.2 and R.sup.3 are identical or different and denote hydrogen or an organic radical, and R.sup.4 and R.sup.5, together with the atoms bearing them, form a monocyclic, bicyclic or tricyclic heterocyclic ring system having 3 to 15 carbon atoms, which process comprises reacting compounds of the formula II defined in the description with compounds of the formula III defined in the description, in the presence of alkanephosphonic anhydrides, where appropriate eliminating radicals which have been introduced to protect other functional groups and, where appropriate, esterifying free carboxyl groups in a manner known per se.

    摘要翻译: 本发明涉及一种制备式I化合物(I)的方法,其中n为1或2,R表示氢或有机基团,R1表示有机基团,R2和R3相同或不同 并且表示氢或有机基团,并且R 4和R 5与带有它们的原子一起形成具有3至15个碳原子的单环,双环或三环杂环体系,该方法包括使在说明书中定义的式II化合物 在描述中定义的式III化合物,在烷基膦酸酐存在下,在适当的情况下,消除已经引入以保护其它官能团的基团,并且在适当的情况下,以本身已知的方式酯化游离羧基。

    Process and test kit for determining free active compounds in biological
fluids
    7.
    发明授权
    Process and test kit for determining free active compounds in biological fluids 失效
    用于测定生物液体中游离活性化合物的方法和测试试剂盒

    公开(公告)号:US06103486A

    公开(公告)日:2000-08-15

    申请号:US75832

    申请日:1993-06-14

    摘要: A method for determining the concentration of the free fraction of an active compound, present in a biological fluid, in the presence of natural binders, the free and bound fractions of the active compound being in mutual equilibrium, bya) contacting a sample of the fluid with an unlabeled antibody,b) separating the sample from the unlabeled antibody,c) incubating the unlabeled antibody with a labeled substance (tracer) for cross-reaction with the antibody andd) measuring the amount of the tracer which is or is not bound to the antibody and calculating from this the concentration of the free fraction of the active compound,wherein the quantity of the unlabeled antibody and/or its affinity for the active compound are so small that they do not substantially effect the equilibrium between the free and bound fractions of the active compound, and the affinity of the tracer for the antibody is substantially higher or substantially lower than that of the active compound itself, and a test kit suitable for this method.

    摘要翻译: 在天然粘合剂存在下,确定存在于生物流体中的活性化合物的游离级分浓度的方法,所述活性化合物的游离和结合级分是相互平衡的,所述方法是通过以下步骤: 具有未标记抗体的液体,b)从未标记的抗体中分离样品,c)将未标记的抗体与标记物质(示踪剂)孵育以与抗体交叉反应,以及d)测量示踪剂的量或不是 与抗体结合,从此计算活性化合物的游离级分的浓度,其中未标记的抗体的量和/或其对活性化合物的亲和力如此之小,使得它们基本上不影响游离和 活性化合物的结合部分,示踪剂对抗体的亲和力显着高于或显着低于活性化合物本身的亲和力, t kit适用于此方法。

    Process for the preparation of n octahydropenta (6) pyrrole carboxylates
    10.
    发明授权
    Process for the preparation of n octahydropenta (6) pyrrole carboxylates 失效
    制备N-甲基吗啉的方法(6)羧甲基纤维素

    公开(公告)号:US5068351A

    公开(公告)日:1991-11-26

    申请号:US560004

    申请日:1990-07-27

    CPC分类号: C07K5/0222

    摘要: The invention relates to a process for the preparation of compounds of the formula I ##STR1## in which n is 1 or 2, R denotes hydrogen or an organic radical, R.sup.1 denotes an organic radical, R.sup.2 and R.sup.3 are identical or different and denote hydrogen or an organic radical, and R.sup.4 and R.sup.5, together with the atoms bearing them, form a monocyclic, bicyclic or tricyclic heterocyclic ring system having 5 to 15 carbon atoms, which process comprises reacting compounds of the formula II defined in the description with compounds of the formula IV defined in the description, in the presence of phosphinic anhydrides of the formula III, where appropriate eliminating radicals which have been introduced to protect other functional groups and, where appropriate, esterifying free carboxyl groups in a manner known per se.

    摘要翻译: 本发明涉及一种制备式I化合物(I)的方法,其中n为1或2,R表示氢或有机基团,R1表示有机基团,R2和R3相同或不同 并且表示氢或有机基团,并且R 4和R 5与带有它们的原子一起形成具有5至15个碳原子的单环,双环或三环杂环体系,该方法包括使在描述中定义的式II化合物 在描述中定义的式IV化合物,在式III的次膦酸酐存在下,其中适当地除去已经引入以保护其它官能团的基团,并且在适当的情况下以本身已知的方式酯化游离羧基 。