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    • 7. 发明授权
    • Dioxaphosphorinanes, their preparation and use for resolving optically
active compounds
    • 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
    • US4814477A
    • 1989-03-21
    • US65121
    • 1987-06-19
    • Hans WijnbergWolter T. Hoeve
    • Hans WijnbergWolter T. Hoeve
    • C07B57/00C07B31/00C07C67/00C07F9/6574C07F9/21
    • C07F9/65744C07F9/65742
    • 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.
    • 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。