Catalytic process for preparing the alkyl esters of ibuprofen
    9.
    发明授权
    Catalytic process for preparing the alkyl esters of ibuprofen 失效
    用于制备布洛芬烷基酯的催化方法

    公开(公告)号:US5315027A

    公开(公告)日:1994-05-24

    申请号:US62906

    申请日:1993-05-11

    IPC分类号: C07C67/36 C07C69/76

    CPC分类号: C07C67/36

    摘要: A process for preparing alkyl esters of ibuprofen is provided. A 1-halo-1-(4-isobutylphenyl)ethane is reacted in an anhydrous medium with carbon monoxide in the presence of an alkoxide source at a temperature between about 10.degree. C. and about 200.degree. C. An excess of several moles of alcohol is preferred. An acid such as hydrogen chloride may also be added. As catalyst, a palladium compound having at least one acid-stable ligand is present; however, an excess of ligand over palladium is advantageous.

    摘要翻译: 提供了制备布洛芬烷基酯的方法。 1-卤代-1-(4-异丁基苯基)乙烷在无水介质中与一氧化碳在醇盐源的存在下在约10℃至约200℃的温度下反应。过量数摩尔 优选酒精。 还可以加入酸如氯化氢。 作为催化剂,存在具有至少一个酸稳定配体的钯化合物; 然而,过量的配体在钯上是有利的。

    Enantiomeric resolution
    10.
    发明授权
    Enantiomeric resolution 失效
    对映体分辨率

    公开(公告)号:US5248813A

    公开(公告)日:1993-09-28

    申请号:US960660

    申请日:1992-10-14

    IPC分类号: C07B57/00 C07C51/487

    CPC分类号: C07C51/487 C07B57/00

    摘要: A process for obtaining a substantially pure enantiomer of an aryl-substituted aliphatic carboxylic acid is described. The process utilizes first an enantiomerically enriched mixture the of aryl-substituted aliphatic carboxylic acid obtained from kinetic resolution, diastereomeric crystallization or asymmetric synthesis processes. This enriched mixture is reacted with a base producing a salt that has the following properties:(1) has at least one eutectic point;(2) a composition that is not at the eutectic point; and(3) a eutectic composition that is closer to the racemic composition than is the eutectic composition of said aryl-substituted carboxylic acid.Substantially pure, enantiomeric salt is separated, leaving a mother liquor comprising the solvent and aryl-substituted aliphatic carboxylic acid enriched in the other enantiomer.

    摘要翻译: 描述了获得芳基取代的脂肪族羧酸的基本上纯的对映异构体的方法。 该方法首先利用从动力学拆分,非对映体结晶或不对称合成方法获得的芳基取代的脂族羧酸的对映体富集混合物。 该富集的混合物与产生具有以下性质的盐的碱反应:(1)具有至少一个共晶点; (2)不在共晶点的组成; 和(3)比所述芳基取代的羧酸的共晶组成更接近外消旋组合物的共晶组合物。 分离基本上纯的对映异构体盐,留下含有溶剂的母液和富集在另一对映异构体中的芳基取代的脂族羧酸。