Racemization and enantiomer separation of clopidogrel
    7.
    发明授权
    Racemization and enantiomer separation of clopidogrel 失效
    氯吡格雷的外消旋化和对映异构体分离

    公开(公告)号:US06800759B2

    公开(公告)日:2004-10-05

    申请号:US10392601

    申请日:2003-03-19

    IPC分类号: C07D4702

    摘要: Processes for separation of enantiomers of clopidogrel, and converting one enantiomer of clopidogrel to another enantiomer of clopidogrel are provided. The enantiomers are separated by crystallizing the (S) enantiomer as camphor sulfonate salt from a hydrocarbon, or a mixture of a hydrocarbon and a co-solvent, preferably DMF:toluene. The (R) enantiomer is then racemized and recycled by reaction with a catalytic amount of a base, preferably with t-butoxide.

    摘要翻译: 提供氯吡格雷的对映异构体分离方法,将氯吡格雷的一种对映异构体转化为氯吡格雷的另一种对映异构体。 通过从烃或烃和共溶剂,优选DMF:甲苯的混合物中结晶(S)对映异构体作为樟脑磺酸盐分离对映异构体。 然后将(R)对映异构体外消旋化并通过与催化量的碱,优选与叔丁醇反应而再循环。

    Process for the synthesis of nabumetone
    8.
    再颁专利
    Process for the synthesis of nabumetone 失效
    合成萘丁酮的方法

    公开(公告)号:USRE37813E1

    公开(公告)日:2002-08-06

    申请号:US09547936

    申请日:2000-04-11

    IPC分类号: C07C4565

    摘要: New process for the synthesis of the antiinflammatory drug known as nabumetone that consists in reacting 2-acetyl-5-bromo-6-methoxynaphthalene with an alkyl acetate in presence of an alkaline alcoholate to get 4-(5-bromo-6-methoxy-2-naphthyl)-4-hydroxybut-3-en-2-one that by catalytic hydrogenation in a polar solvent and in presence of a base gives 4-(6-methoxy-2-naphthyl)butan-2-one known as nabumetone.

    摘要翻译: 用于合成称为萘丁美酮的抗炎药物的新方法,其包括使2-乙酰基-5-溴-6-甲氧基萘与乙酸烷基酯在碱性醇化物存在下反应,得到4-(5-溴-6-甲氧基 - 2-萘基)-4-羟基丁-3-烯-2-酮,通过极性溶剂中的催化氢化和碱的存在,得到4-(6-甲氧基-2-萘基)丁-2-酮,称为萘丁酮 。