Racemization of precursors to levobupivacaine and analogues thereof
    1.
    发明授权
    Racemization of precursors to levobupivacaine and analogues thereof 有权
    左布比卡因及其类似物的前体外消旋化

    公开(公告)号:US6156900A

    公开(公告)日:2000-12-05

    申请号:US250473

    申请日:1999-02-12

    CPC分类号: C07D211/60 C07B55/00

    摘要: A process for the preparation of optically-enriched pipecolic acid as a salt with an optically-active acid, comprises asymmetric transformation of pipecolic acid, as a racemic mixture of a mixture enriched in the opposite enantiomer from that desired, with the optically-active acid in a solvent comprising an acid that causes racemisation, in the absence of aldehyde.

    摘要翻译: 用光学活性酸制备作为盐的光学富含哌啶酸的方法包括使用光学活性酸作为富含相反对映异构体的混合物的外消旋混合物的哌啶酸的不对称转化 在包含无醛的情况下引起外消旋化的酸的溶剂中。

    Method for preparation of aryl substituted alefinic secondary amino
compounds
    5.
    发明授权
    Method for preparation of aryl substituted alefinic secondary amino compounds 失效
    芳基取代的烯烃仲氨基化合物的制备方法

    公开(公告)号:US5663356A

    公开(公告)日:1997-09-02

    申请号:US635165

    申请日:1996-04-23

    CPC分类号: C07D213/38 C07D213/61

    摘要: Patients susceptible to or suffering from central nervous system are treated by administering an effective amount of an aryl substituted olefinic amine compound, such as (E)-metanicotine. (E)-metanicotine is provided from nicotine. Nicotine is reacted with ethyl chloroformate to produce ethyl N-methyl-N-[4-chloro-4-(3-pyridyl)butyl]carbamate, which then is reacted in the presence of potassium tert-butoxide, tetrahydrofuran and dimethylformamide to produce (E)-metanicotine N-ethyl carbamate, which then is subjected to hydrolysis using hydrochloric acid to produce a reaction mixture containing (E)-metanicotine. The reaction mixture containing (E)-metanicotine is adjusted to a slightly basic pH, and then contacted with dichloromethane. The resulting water immiscible phase then is separated from the aqueous phase. The aqueous phase, then is adjusted to a very basic pH, and then contacted with methyl tert-butyl ether. (E)-metanicotine is taken up by the methyl tert-butyl ether, and after separation of the methyl tert-butyl ether from the aqueous phase, the desired product is separated from the methyl tert-butyl ether.

    摘要翻译: 通过施用有效量的芳基取代的烯烃胺化合物(例如(E) - 亚硝酸)来治疗患有中枢神经系统或患有中枢神经系统的患者。 (E) - 西尼可因由尼古丁提供。 使尼古丁与氯甲酸乙酯反应生成N-甲基-N- [4-氯-4-(3-吡啶基)丁基]氨基甲酸乙酯,然后在叔丁醇钾,四氢呋喃和二甲基甲酰胺的存在下反应,生成( E) - 氰胺基胺N-乙基氨基甲酸酯,然后用盐酸进行水解,得到含有(E) - 间苯胺的反应混合物。 将含有(E) - 间苯胺的反应混合物调节至略微碱性的pH,然后与二氯甲烷接触。 然后将所得的水不混溶相与水相分离。 然后将水相调节至非常碱性的pH,然后与甲基叔丁基醚接触。 (E) - 间苯虫胺被甲基叔丁基醚吸收,甲基叔丁基醚从水相中分离后,将所需产物与甲基叔丁基醚分离。