Compounds useful in enzymatic resolution systems and their preparation
    67.
    发明授权
    Compounds useful in enzymatic resolution systems and their preparation 失效
    可用于酶解体系及其制备的化合物

    公开(公告)号:US5196568A

    公开(公告)日:1993-03-23

    申请号:US178735

    申请日:1988-04-07

    摘要: This invention relates to novel compositions of matter which are esters with enhanced water solubility, for use in aqueous enzymatic resolution reactions of racemic mixtures of these esters for producing the separate chiral isomers of the racemic mixture. The invention also relates to novel methods for preparing these esters. The importance of the production of the separate chiral isomers of the racemic mixtures resides in the isolation of the isomers which frequently have different biological activities. Of particular significance regarding the water soluble esters of this invention is that they are derivatized with groups which enhance their aqueous solubility and their reactivity with enzymatic resolving methods which are mediated in an aqueous environment. In addition, the importance of these compounds resides in their being useful in novel methods for facilitating the enzymatic resolution reactions of racemic mixtures of esters, which are derivatized with groups which enhance the esters' aqueous solubility, in 1) a homogeneous aqueous reaction system where an extractive phase is not present, 2) a multiphase dispersion extractive reaction where an extractive phase is present, and 3) an extractive membrane reactor where the enzyme is placed alternatively either (a) in the aqueous phase, (b) in association with the membrane, or (c) in the aqueous phase and in association with the membrane, wherein the aqueous ester phase is contacted with one side of the membrane, and where an organic extractive phase is contacted with the other side of the membrane, wherein the extractive phase serves to remove the resolving reaction product.

    摘要翻译: 本发明涉及物质的新型组合物,其是具有增强的水溶性的酯,用于这些酯的外消旋混合物的水性酶拆分反应中用于产生外消旋混合物的分离的手性异构体。 本发明还涉及制备这些酯的新方法。 外消旋混合物的分离手性异构体的生产的重要性在于分离经常具有不同生物活性的异构体。 对于本发明的水溶性酯具有特别意义的是它们用增强其水溶性的基团和它们与在水性环境中介导的酶拆分方法的反应性的基团衍生化。 此外,这些化合物的重要性在于它们可用于促进酯的外消旋混合物的酶拆分反应的新方法,其通过增强酯的水溶性的基团衍生化,在1)均匀的水反应体系中,其中 萃取相不存在,2)存在萃取相的多相分散萃取反应,和3)提取膜反应器,其中酶在(a)在水相中交替放置,(b)与 膜或(c)在水相中并与膜结合,其中酯水相与膜的一侧接触,并且其中有机萃取相与膜的另一侧接触,其中提取物 相用于除去分解反应产物。