Sesquihydrate of naphthyridine derivative, and process for the
preparation thereof
    6.
    发明授权
    Sesquihydrate of naphthyridine derivative, and process for the preparation thereof 失效
    萘啶衍生物的倍半水合物及其制备方法

    公开(公告)号:US4442101A

    公开(公告)日:1984-04-10

    申请号:US345916

    申请日:1982-02-04

    摘要: Novel 1-ethyl-6-fluoro-1,4-dihyono-4-oxo -7-(1-piperazinyl)-1,8-naphthyridine-3-carboxylic acid.sesquihydrate (ATT-2266.sesquihydrate). The aforesaid compound can be prepared by heating 1-ethyl-6-fluoro-1,4-dihydro-4-oxo -7-(1-piperazinyl)-1,8-naphthyridine-3-carboxylic acid at a temperature above about 60.degree. C. in the presence of water in an amount sufficient to form the sesquihydrate. This sesquihydrate is much more stable than the anhydrate and the trihydrate and is superior to the anhydrate in the rate of dissolution and transference into the body through the intestines. Thus, it is especially useful as a pharmaceutical compound.

    摘要翻译: 新的1-乙基-6-氟-1,4-二氢化-4-氧代-7-(1-哌嗪基)-1,8-萘啶-3-羧酸二水合物(ATT-2266,水合二水合物)。 上述化合物可以通过在高于约60℃的温度下加热1-乙基-6-氟-1,4-二氢-4-氧代-7-(1-哌嗪基)-1,8-二氮杂萘-3-羧酸来制备 在水存在下,其量足以形成倍半水合物。 这种倍半水合物比无水物和三水合物更稳定,并且在溶解速率和通过肠中转移到体内优于无水物质。 因此,作为药物化合物是特别有用的。