Alpha-fluoro alkynoic acids with anticonvulsant activity
    4.
    发明授权
    Alpha-fluoro alkynoic acids with anticonvulsant activity 失效
    具有抗惊厥活性的α-氟代炔酸

    公开(公告)号:US06184401B2

    公开(公告)日:2001-02-06

    申请号:US09337912

    申请日:1999-06-22

    Applicant: Heinz Nau

    Inventor: Heinz Nau

    Abstract: Alpha-fluorinated alkynoic acids and pharmaceutical compositions containing these compounds are provided, which are useful for the treatment and prevention of seizures such as are associated with epilepsy. The compounds of the invention exhibit reduced side effects, relative to valproic acid, with regard to sedation and teratogenic potential.

    Abstract translation: 提供了α-氟代炔酸和含有这些化合物的药物组合物,其可用于治疗和预防与癫痫相关的癫痫发作。 相对于丙戊酸,本发明的化合物在镇静和致畸潜能方面表现出减少的副作用。

    Process for preparing methyl 4-oxo-5-tetradecynoate
    5.
    发明授权
    Process for preparing methyl 4-oxo-5-tetradecynoate 失效
    4-氧代-5-十四碳酸甲酯的制备方法

    公开(公告)号:US4808340A

    公开(公告)日:1989-02-28

    申请号:US136041

    申请日:1987-12-21

    CPC classification number: C07C69/606

    Abstract: A process for preparing methyl 4-oxo-5-tetradecynoate useful as an intermediate for synthesizing (R,Z)-5-dec-1-enyl-oxacyclopentan-2-one, which comprises reacting monomethyl succinate with an alkyl chlorocarbonate in the presence of a base to form an acid anhydride and reacting the acid anhydride with a Grignard reagent of 1-decyne. Methyl 4-oxo-5-tetradecynoate can be prepared in high yields at high purities by this process.

    Abstract translation: 用作合成(R,Z)-5-癸-1-烯基 - 氧环戊烷-2-酮的中间体的4-氧代-5-十四碳酸甲酯的制备方法,其包括在存在下使琥珀酸甲酯与氯代碳酸烷基酯反应 的碱形成酸酐,并使酸酐与1-癸炔的格利雅试剂反应。 通过该方法可以高纯度的高产率制备4-氧代-5-十四碳酸甲酯。

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