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    Crystalline substance of cefditoren pivoxyl and the production of the same
    1.
    发明授权
    Crystalline substance of cefditoren pivoxyl and the production of the same 有权
    头孢托仑的新型结晶物质及其生产

    公开(公告)号：US06294669B1

    公开(公告)日：2001-09-25

    申请号：US09269109

    申请日：1999-03-19

    申请人： Kiyoshi Yasui ,  Masahiro Onodera ,  Masamichi Sukegawa ,  Tatsuo Watanabe ,  Yuichi Yamamoto ,  Yasushi Murai ,  Katsuharu Iinuma

    发明人： Kiyoshi Yasui ,  Masahiro Onodera ,  Masamichi Sukegawa ,  Tatsuo Watanabe ,  Yuichi Yamamoto ,  Yasushi Murai ,  Katsuharu Iinuma

    IPC分类号： C07D50124

    CPC分类号： C07D501/00

    摘要： As a novel substance is provided such a new, crystalline substance of Cefditoren povoxyl which has a high purity and an enhanced thermal stability on storage. This crystalline Cefditoren pivoxyl may be prepared by a process comprising a step of dissolving amorphous substance of Cefditoren pivoxyl in an anhydrous, first organic solvent capable of dissolving said amorphous substance well therein, and steps of replacing the first organic solvent component of the resulting solution by an anhydrous alkanol of 1 to 5 carbon atoms as a second organic solvent, in such a manner that the firstly prepared solution of Cefditoren pivoxyl in the first organic solvent is mixed with a volume of the alkanol and then is concentrated below 15° C. under reduced pressure, and so on. Thereby, the process proceeds so as to produce a solution containing 50 mg/ml to 250 mg/ml of Cefditoren pivoxyl dissolved in the alkanol alone. From the latter solution, crystals of Cefditoren pivoxyl are induced to deposit by addition of water at a temperature of 0-10° C. The resulting admixture of the concentrated solution of Cefditoren pivoxyl in alkanol with added water and the deposited Cefditoren pivoxyl is then agitated 10° C. or below, to effect a complete crystallization of Cefditoren pivoxyl.

    摘要翻译： 作为一种新物质，提供了这样一种具有高纯度和增加的储存热稳定性的新型头孢托仑聚氧乙烯醚的结晶物质。 这种结晶的头孢托仑新戊基可以通过包括以下步骤的方法来制备，所述方法包括将能够将所述无定形物质溶解在其中的无水的第一有机溶剂中溶解新戊酰氧基甲基头孢托仑的无定形物质，以及将所得溶液的第一有机溶剂组分置换为 将具有1至5个碳原子的无水链烷醇作为第二有机溶剂，使得将首先制备的在第一有机溶剂中的新戊酰氧基头孢托仑的溶液与一定体积的链烷醇混合，然后在15℃以下浓缩 减压等。 由此，进行处理，从而产生溶解在单独的链烷醇中的含有50mg / ml〜250mg / ml的新戊酰氧基甲基头孢地托仑的溶液。 从后一种溶液中，通过在0-10℃的温度下，通过加入水诱导新戊酸头孢托仑的晶体沉淀。然后搅拌所得的新戊酰氧基甲基头孢地托仑在链烷醇中与加入的水的混合物和沉积的新戊糖酯 10℃或更低，以实现新戊酰氧基甲基头孢托仑的完全结晶。

    Crystalline substance of cefditoren pivoxyl and the production of the same
    2.
    发明授权
    Crystalline substance of cefditoren pivoxyl and the production of the same 有权
    头孢托仑的新型结晶物质及其生产

    公开(公告)号：US06441162B2

    公开(公告)日：2002-08-27

    申请号：US09854462

    申请日：2001-05-15

    申请人： Kiyoshi Yasui ,  Masahiro Onodera ,  Masamichi Sukegawa ,  Tatsuo Watanabe ,  Yuichi Yamamoto ,  Yasushi Murai ,  Katsuharu Iinuma

    发明人： Kiyoshi Yasui ,  Masahiro Onodera ,  Masamichi Sukegawa ,  Tatsuo Watanabe ,  Yuichi Yamamoto ,  Yasushi Murai ,  Katsuharu Iinuma

    IPC分类号： C07D50124

    CPC分类号： C07D501/00

    摘要： A crystalline substance of Cefditoren pivoxyl is provided which has a high purity and enhanced thermal stability on storage. This crystalline Cefditoren pivoxyl may be prepared by a process comprising a step of dissolving an amorphous form of Cefditoren pivoxyl in an anhydrous, first organic solvent capable of dissolving said amorphous form well therein, and steps of replacing the first organic solvent component of the resulting solution by an anhydrous alkanol of 1 to 5 carbon atoms as a second organic solvent, in such a manner that the firstly prepared solution of Cefditoren pivoxyl in the first organic solvent is mixed with a volume of the alkanol and then is concentrated below 15° C. under reduced pressure, and so on. Thereby, the process proceeds so as to produce a solution containing 50 mg/ml to 250 mg/ml of Cefditoren pivoxyl dissolved in the alkanol alone. From the latter solution, crystals of Cefditoren pivoxyl are induced to deposit by addition of water at a temperature of 0-10° C. The resulting admixture of the concentrated solution of Cefditoren pivoxyl in alkanol with added water and the deposited Cefditoren pivoxyl is then agitated 10° C. or below, to effect a complete crystallization of Cefditoren pivoxyl.

    摘要翻译： 提供了新戊酸头孢托仑的结晶物质，其具有高纯度和增强的储存热稳定性。 这种结晶的头孢托仑新戊基可以通过包括以下步骤的方法来制备，该方法包括将无定形形式的新戊酰氧基头孢托仑溶解在能够将所述无定形形式溶解在其中的无水第一有机溶剂中，以及将所得溶液的第一有机溶剂组分 通过具有1至5个碳原子的无水链烷醇作为第二有机溶剂，使得将首先制备的在第一有机溶剂中的新戊酰氧基头孢托仑的溶液与一定体积的链烷醇混合，然后浓缩至15℃以下。 减压下等。 由此，进行处理，从而产生溶解在单独的链烷醇中的含有50mg / ml〜250mg / ml的新戊酰氧基甲基头孢地托仑的溶液。 从后一种溶液中，通过在0-10℃的温度下，通过加入水诱导新戊酸头孢托仑的晶体沉淀。然后搅拌所得的新戊酰氧基甲基头孢地托仑在链烷醇中与加入的水的混合物和沉积的新戊糖酯 10℃或更低，以实现新戊酰氧基甲基头孢托仑的完全结晶。