Process for the racemization of optically active 1-aryl-alkylamines
    7.
    发明授权
    Process for the racemization of optically active 1-aryl-alkylamines 失效
    光活性1-芳基 - 氨基甲酸酯的制备方法

    公开(公告)号:US5183939A

    公开(公告)日:1993-02-02

    申请号:US796109

    申请日:1991-11-21

    CPC分类号: C07C209/68 C07B2200/07

    摘要: A new process for the racemization of optically active 1-aryl-alkylamines of the formula (I) ##STR1## in which Ar represents optionally substituted aryl andR represents alkyl,which is characterized in that compounds of the formula (I) which largely have the R- or S-configuration at the carbon atom marked by * are reacted with metal alkoxides in dimethyl sulphoxide, optionally in the presence of appropriate alcohols, at temperatures between 0.degree. C. and 200.degree. C.

    摘要翻译: 用于使式(I)的光学活性1-芳基 - 烷基胺外消旋化的新方法其中Ar表示任选取代的芳基,R表示烷基,其特征在于式(I)化合物 在0℃和200℃之间的温度下,在由*标记的碳原子上大部分具有R-或S-构型的金属醇盐在二甲基亚砜中任选地在适当的醇存在下与二甲基亚砜反应。

    Process for working up the crystallization mother liquor from the
resolution of the racemate of 1-(4-chlorophenyl)-ethylamine
    8.
    发明授权
    Process for working up the crystallization mother liquor from the resolution of the racemate of 1-(4-chlorophenyl)-ethylamine 失效
    从1-(4-氯苯基) - 乙酰胺的化合物的分解中加工结晶母液的方法

    公开(公告)号:US5144077A

    公开(公告)日:1992-09-01

    申请号:US798678

    申请日:1991-11-26

    CPC分类号: C07C209/88

    摘要: The invention relates to a process for working up to crystallization mother liquor which is obtained in the resolution of the racemate of 1-(4-chlorophenyl)-ethylamine of the formula (I) with S-(-)-N-phenylcarbamoyllactic acid of the formula (II) by removing the ethanol from the ethanolic crystallization mother liquor by distillation in a 1st step and stirring the residue which remains with tert.-butyl methyl ether or toluene in a second step and it being possible to employ the resulting crystalline salt of (R/S)-1-(4-chlorophenyl)-ethylamine and (S)-(-)-N-phenylcarbamoyllactic acid directly again for the resolution of the racemate. The (S)-form of the amine is mainly present in the mother liquor and can be racemised and added to the resolution of the racemate again.

    摘要翻译: 本发明涉及一种用于处理结晶母液的方法,该方法是用式(I)的1-(4-氯苯基) - 乙胺的外消旋物与S-( - ) - N-苯基氨基甲酰基乳酸的拆分得到的 通过在第一步骤中蒸馏从乙醇结晶母液中除去乙醇并在第二步骤中搅拌残余物与叔丁基甲基醚或甲苯残留的式(II),并且可以使用所得到的结晶盐 的(R / S)-1-(4-氯苯基) - 乙胺和(S) - ( - ) - N-苯基氨基甲酰基乳酸直接用于拆分外消旋体。 胺的(S)形式主要存在于母液中,并且可以外消旋化并再次添加到外消旋物的分辨率中。