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    Process for the preparation of cyclic N-hydroxydicarboximides
    3.
    发明授权
    Process for the preparation of cyclic N-hydroxydicarboximides 失效
    环状N-羟基二酰亚胺的制备方法

    公开(公告)号：US06316639B1

    公开(公告)日：2001-11-13

    申请号：US09657201

    申请日：2000-09-07

    申请人： Elke Fritz-Langhals

    发明人： Elke Fritz-Langhals

    IPC分类号： C07D20746

    CPC分类号： C07D209/48 ,  C07D221/14 ,  C07D487/04

    摘要： The invention discloses a process for the preparation of cyclic N-hydroxydicarboximides, involving reacting a dicarboxylic acid or anhydride thereof with a salt of hydroxylamine in solution without the further addition of a base.

    摘要翻译： 本发明公开了一种环状N-羟基二酰亚胺的制备方法，包括使二羧酸或其酸酐与溶液中的羟胺盐反应而不需要进一步添加碱。

    Synthesis of a novel paramagnetic amino derivative (epm-5) for labelling chemical and biological macromolecules
    4.
    发明授权
    Synthesis of a novel paramagnetic amino derivative (epm-5) for labelling chemical and biological macromolecules 失效
    用于标记化学和生物大分子的新型顺磁性氨基衍生物（epm-5）的合成

    公开(公告)号：US06797829B1

    公开(公告)日：2004-09-28

    申请号：US10018842

    申请日：2001-12-21

    申请人： Clóvis Ryuichi Nakaie ,  Mineko Tominaga ,  Antonio Cechlli Matto Paiva ,  Simone dos Reis Barbosa ,  Reinaldo Machetto ,  Shirley Schreier

    发明人： Clóvis Ryuichi Nakaie ,  Mineko Tominaga ,  Antonio Cechlli Matto Paiva ,  Simone dos Reis Barbosa ,  Reinaldo Machetto ,  Shirley Schreier

    IPC分类号： C07D20746

    CPC分类号： C07D207/46 ,  Y02P20/55

    摘要： The present invention refers to the synthesis and application of 2,2,5,5-tetramethylpyrrolidine-N-oxyl-(9-fluorenylmethyloxycarbonyl)-3-amine-4-carboxylic acid, a novel paramagnetic amino acid derivative (spin label), denominated Fmoc-Poac. Fmoc-Poac can be coupled to peptide sequences and other molecules or systems. It can be inserted anywhere in a peptide segment, even at an internal position if necessary, after removal of its temporary amine protecting group, Fmoc. Owing to its pyrrolidine structure, this molecule may induce differentiated conformations as compared with normal &agr;-amino acids, thus being a valuable probe for structural-biological activity of several relevant peptides. The Poac-angiotensin II analogue was synthesized as a model according to its use as a chemical derivative.

    摘要翻译： 本发明涉及2,2,5,5-四甲基吡咯烷-N-氧基 - （9-芴基甲氧基羰基）-3-胺-4-羧酸（新型顺磁性氨基酸衍生物（自旋标记））的合成和应用， 称为Fmoc-Poac。 Fmoc-Poac可以与肽序列和其他分子或系统偶联。 除去其临时胺保护基团Fmoc之外，如果需要，它可以插入肽段的任何地方，甚至在内部位置。 由于其吡咯烷结构，与正常的α-氨基酸相比，该分子可诱导分化的构象，因此是几种相关肽的结构 - 生物活性的有价值的探针。 根据其作为化学衍生物的用途合成了Poac-血管紧张素II类似物作为模型。

    Process for preparing pyrrolidone derivative
    5.
    发明授权
    Process for preparing pyrrolidone derivative 有权
    吡咯烷酮衍生物的制备方法

    公开(公告)号：US06429316B1

    公开(公告)日：2002-08-06

    申请号：US09447237

    申请日：1999-11-23

    申请人： Kazunari Takahashi ,  Yoko Seto ,  Masaru Utsunomiya ,  Souichi Orita ,  Kazutaka Maruyama ,  Tomonori Okubi

    发明人： Kazunari Takahashi ,  Yoko Seto ,  Masaru Utsunomiya ,  Souichi Orita ,  Kazutaka Maruyama ,  Tomonori Okubi

    IPC分类号： C07D20746

    CPC分类号： C07D207/267

    摘要： Disclosed is a process for preparing a pyrrolidone derivative, which comprises allowing at least one of &ggr;-butyrolactone, 4-hydroxybutyric acid, and a low-molecular polymer of 4-hydroxybutyric acid to react with an alkylamine, wherein (i) the content of a primary amine in said alkylamine is 85% by weight or lower, and (ii) the molar ratio of the total amount of the charged primary and secondary amines to the total amount of the charged &ggr;-butyrolactone, 4-hydroxybutyric acid, and low-molecular 4-hydroxybutyric acid polymers satisfies formula: 1.0≦(A1+A2/2.5)/(B1+B2+B3) wherein A1, A2, B1, B2, and B3 represent the molar amounts of a primary amine, a secondary amine, &ggr;-butyrolactone, 4-hydroxybutyric acid, and low-molecular 4-hydroxybutyric acid polymers, respectively.

    摘要翻译： 公开了一种制备吡咯烷酮衍生物的方法，其包括使γ-丁内酯，4-羟基丁酸和4-羟基丁酸的低分子量聚合物中的至少一种与烷基胺反应，其中（i） 所述烷基胺中的伯胺为85重量％以下，（ii）带电荷的伯胺与仲胺的总量相对于带电量的γ-丁内酯，4-羟基丁酸的总量的摩尔比为低 分子式4-羟基丁酸聚合物满足式：其中A1，A2，B1，B2和B3代表伯胺，仲胺，γ-丁内酯，4-羟基丁酸和低分子量的4-羟基丁酸的摩尔量 酸聚合物。