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    Process for the separation of a mixture of enantiomers
    5.
    发明授权
    Process for the separation of a mixture of enantiomers 失效
    分离对映异构体混合物的方法

    公开(公告)号：US06235927B1

    公开(公告)日：2001-05-22

    申请号：US08955612

    申请日：1997-10-22

    申请人： Ton R. Vries ,  Hans Wijnberg ,  Erik Van Echten ,  Lumbertus A. Hulshof ,  Quirinus B. Broxterman

    发明人： Ton R. Vries ,  Hans Wijnberg ,  Erik Van Echten ,  Lumbertus A. Hulshof ,  Quirinus B. Broxterman

    IPC分类号： C07B5500

    CPC分类号： C07D295/023 ,  C07B57/00 ,  C07C51/487 ,  C07C209/80 ,  C07C213/10 ,  C07C227/34 ,  C07C253/34 ,  C07C2602/08 ,  C07F9/65742 ,  C07C211/27 ,  C07C211/28 ,  C07C211/29 ,  C07C215/08 ,  C07C215/44 ,  C07C215/50 ,  C07C229/34 ,  C07C229/36 ,  C07C255/42

    摘要： A diastereomer complex obtained via a process for the separation of enantiomers is disclosed, wherein separation can be rapidly effected such that enantiomers are obtained with high e.e. values. The process pets the separation of mixtures of enantiomers in which more than one resolving agent is used, of which at least one resolving agent is optically active, and which yields a diastereomer complex containing at least two resolving agents in optically active form. The process provides for, inter alia, a diastereomer complex having at least three compounds of which at least two compounds are resolving agents in optically active form, and at least one compound is an onantiomer in optically active form. Also provided is a diastereomer complex having at least three compounds of which at lea one compound is a resolving agent in optically active form, and at least two compounds which are enantiomers in optically active form.

    摘要翻译： 公开了通过分离对映异构体的方法获得的非对映异构体复合物，其中可快速进行分离，使得以高e.e。获得对映异构体。 价值观。 该方法可以分离其中使用多于一种拆分剂的对映异构体混合物，其中至少一种拆分剂是光学活性的，并且其产生含有至少两种旋光活性形式的拆分剂的非对映异构体复合物。 该方法特别提供了具有至少三种化合物的非对映异构体复合物，其中至少两种化合物是旋光活性形式的拆分剂，并且至少一种化合物是光学活性形式的对映异构体。 还提供了具有至少三种化合物的非对映异构体复合物，其中一种化合物是旋光活性形式的拆分剂，以及至少两种为光学活性形式的对映异构体的化合物。

    Dioxaphosphorinanes, their preparation and use for resolving optically active compounds
    7.
    发明授权
    Dioxaphosphorinanes, their preparation and use for resolving optically active compounds 失效
    二氧杂磷杂环丁烷，它们的制备和用于拆分光学活性化合物的用途

    公开(公告)号：US4814477A

    公开(公告)日：1989-03-21

    申请号：US65121

    申请日：1987-06-19

    申请人： Hans Wijnberg ,  Wolter T. Hoeve

    发明人： Hans Wijnberg ,  Wolter T. Hoeve

    IPC分类号： C07B57/00 ,  C07B31/00 ,  C07C67/00 ,  C07F9/6574 ,  C07F9/21

    CPC分类号： C07F9/65744 ,  C07F9/65742

    摘要： A new family of compounds known as dioxaphosphorinanes having the formula: ##STR1## wherein, M represents a hydrogen atom, a metal ion or an ammonium ion; R1 and R2, individually, represents a hydrogen atom, a halogen atom, an alkyl group having from 1 to 4 carbon atoms, an alkoxy group having from 1 to 4 carbon atoms or a nitro group or, together, represent a methylene dioxy group; and R3 and R4, individually, represents a halogen atom, an alkyl group having from 1 to 4 carbon atoms or a hydrogen atom so long as only one of the groups R3 and R4 represents a hydrogen atom or, together, represent a cyclohexyl group.A method for preparing these dioxaphosphorinanes by reacting phosphoryl chloride with a substituted 1-phenyl-1,3-dihydroxypropane is described. Also described is a method for resolving the new dioxaphosphorinanes into their optical isomers by reacting them with an optically active amino-compound. Similarly, a method for resolving the racemates of several amino-compounds, such as hydroxyphenylglycine and phenylalanine, into optically active isomers by reacting with a dioxaphosphorinane is described.

    摘要翻译： 已知为二氧杂磷杂环壬烷的新家族化合物，具有下式：其中M表示氢原子，金属离子或铵离子; R 1和R 2分别表示氢原子，卤素原子，具有1至4个碳原子的烷基，具有1至4个碳原子的烷氧基或硝基，或者一起表示亚甲基二氧基; R 3和R 4各自表示卤素原子，具有1至4个碳原子的烷基或氢原子，只要R3和R4中只有一个表示氢原子，或者一起代表环己基。 描述了通过使磷酰氯与取代的1-苯基-1,3-二羟基丙烷反应来制备这些二氧杂磷杂环丁烷的方法。 还描述了通过使它们与光学活性氨基化合物反应来将新的二氧杂磷杂环丁烷分解成它们的光学异构体的方法。 类似地，描述了将几种氨基化合物如羟基苯基甘氨酸和苯丙氨酸的外消旋体与二氧杂磷杂环丁烷反应转化为旋光异构体的方法。

    Process for the separation of a mixture of enantiomers
    8.
    发明授权
    Process for the separation of a mixture of enantiomers 失效
    分离对映异构体混合物的方法

    公开(公告)号：US06465684B2

    公开(公告)日：2002-10-15

    申请号：US09784083

    申请日：2001-02-16

    申请人： Ton R. Vries ,  Hans Wijnberg ,  Erik Van Echten ,  Lumbertus A. Hulshof ,  Quirinus B. Broxterman

    发明人： Ton R. Vries ,  Hans Wijnberg ,  Erik Van Echten ,  Lumbertus A. Hulshof ,  Quirinus B. Broxterman

    IPC分类号： C07C33100

    CPC分类号： C07D295/023 ,  C07B57/00 ,  C07C51/487 ,  C07C209/80 ,  C07C213/10 ,  C07C227/34 ,  C07C253/34 ,  C07C2602/08 ,  C07F9/65742 ,  C07C211/27 ,  C07C211/28 ,  C07C211/29 ,  C07C215/08 ,  C07C215/44 ,  C07C215/50 ,  C07C229/34 ,  C07C229/36 ,  C07C255/42

    摘要： A diastereomer complex obtained via a process for the separation of enantiomers is disclosed, wherein separation can be rapidly effected such that enantiomers are obtained with high e.e. values. The process permits the separation of mixtures of enantiomers in which more than one resolving agent is used, of which at least one resolving agent is optically active, and which yields a diastereomer complex containing at least two resolving agents in optically active form. The process provides for, inter alia, a diastereomer complex having at least three compounds of which at least two compounds are resolving agents in optically active form, and at least one compound is an enantiomer in optically active form. Also provided is a diastereomer complex having at least three compounds of which at least one compound is a resolving agent in optically active form, and at least two compounds which are enantiomers in optically active form.

    摘要翻译： 公开了通过分离对映异构体的方法获得的非对映异构体复合物，其中可快速进行分离，使得以高e.e。获得对映异构体。 价值观。 该方法允许分离其中使用多于一种拆分剂的对映异构体的混合物，其中至少一种拆分剂是光学活性的，并且其产生含有至少两种光学活性形式的拆分剂的非对映异构体复合物。 该方法特别提供了具有至少三种化合物的非对映异构体复合物，其中至少两种化合物是旋光活性形式的拆分剂，并且至少一种化合物是光学活性形式的对映异构体。 还提供了具有至少三种化合物的至少三种化合物的非对映异构体复合物，其中至少一种化合物是光学活性形式的拆分剂，以及至少两种是光学活性形式的对映异构体的化合物。