Process for preparing pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl amino acids
    9.
    发明授权
    Process for preparing pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl amino acids 有权
    制备N-(1(S) - 乙氧基羰基-3-苯基丙基)-L-丙氨酰氨基酸的药理学可接受盐的方法

    公开(公告)号:US06335453B1

    公开(公告)日:2002-01-01

    申请号:US09269107

    申请日:1999-03-19

    IPC分类号: C07K5062

    CPC分类号: C07K5/0222 C07K5/06026

    摘要: There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine.N-carboxyanhydride under basic condition, carrying out decarboxylation under between neutral and acidic condition to obtain N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid, and forming a pharmacologically acceptable salt thereof, wherein the production of a by-product (3): is suppressed by carrying out in an aqueous liquid a series of operations till formation of the pharmacologically acceptable salt or till isolation of the pharmacologically acceptable salt. The present invention enables to prepare the pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid having high quality, in a commercial scale with high yield and economical efficiency.

    摘要翻译: 提供了制备N-(1(S) - 乙氧基羰基-3-苯基丙基)-L-丙氨酰 - 氨基酸的药学上可接受的盐的方法,其包括将氨基酸和N-(1(S) - 乙氧基羰基 - 3-苯基丙基)-L-丙氨酸N-羧酸酐,在中性和酸性条件下进行脱羧,得到N-(1(S) - 乙氧基羰基-3-苯基丙基)-L-丙氨酰 - 氨基酸,和 形成其药理学上可接受的盐,其中通过在含水液体中进行一系列操作直到形成药理学上可接受的盐或直到药理学上可接受的盐的分离来抑制副产物(3)的产生。 本发明能够以高产率和经济效益以商业规模制备质量高的N-(1(S) - 乙氧基羰基-3-苯基丙基)-L-丙氨酰 - 氨基酸的药理学上可接受的盐。

    Method for producing surfactin and salt thereof
    10.
    发明授权
    Method for producing surfactin and salt thereof 有权
    表面活性素及其盐的制备方法

    公开(公告)号:US08883968B2

    公开(公告)日:2014-11-11

    申请号:US13876734

    申请日:2011-09-30

    CPC分类号: C07K1/145 C07K1/36 C07K7/06

    摘要: The method for producing a surfactin or a salt thereof according to the present invention comprises the steps of adding an organic solvent containing a branched alkyl alcohol to a culture fluid containing the surfactin or the salt thereof, or to a solution obtained by removing an insoluble component from the culture fluid, and extracting the surfactin or the salt thereof with the organic solvent,wherein the surfactin or the salt thereof is represented by the formula (1): wherein * indicates an optically active center; X is an amino acid selected from leucine, isoleucine and valine; R is a C9-13 alkyl group or a C9-13 branched alkyl group; and M is an alkali metal, an alkaline earth metal, an optionally-substituted amine or the like.

    摘要翻译: 本发明的表面活性素或其盐的制造方法包括将含有支链烷基醇的有机溶剂添加到含有所述表面活性素或其盐的培养液中的步骤,或者将除去不溶成分 从所述培养液中提取所述表面活性素或其盐,其中所述表面活性素或其盐由式(1)表示:其中*表示光学活性中心; X是选自亮氨酸,异亮氨酸和缬氨酸的氨基酸; R为C 9-13烷基或C 9-13支链烷基; M是碱金属,碱土金属,任意取代的胺等。