Process for preparing diisopropyl((1-(hydroxymethyl)-cyclopropyl)oxy)methylphosphonate
    2.
    发明授权
    Process for preparing diisopropyl((1-(hydroxymethyl)-cyclopropyl)oxy)methylphosphonate 失效
    制备((1-(羟基甲基) - 环丙基)氧基)甲基膦酸二异丙酯的方法

    公开(公告)号:US07795463B2

    公开(公告)日:2010-09-14

    申请号:US11631263

    申请日:2005-06-27

    IPC分类号: C07F9/40 C07C43/164

    CPC分类号: C07F9/65616 C07F9/4006

    摘要: Disclosed is a process for preparing a compound of the following formula (2): including the steps of reacting a compound of the following formula (4): with trityl chloride to prepare trityloxy-acetic acid ethyl ester of the following formula (8): reacting the compound of formula (8) with ethyl magnesium halide to prepare 1-trityloxymethyl-cyclopropanol of the following formula (9): combining the 1-trityloxymethyl-cyclopropanol of formula (9) with diisopropylbromo-methylphosphonate in a solvent in the presence of a base to prepare (1-trityloxymethyl-cyclopropoxymethyl)-phosphonic acid diisopropyl ester of the following formula (10): as a solid form, and converting the trityl group of the compound of formula (10) into a hydroxyl group.

    摘要翻译: 公开了下述式(2)的化合物的制备方法:包括使下述式(4)的化合物与三苯甲基氯反应,制备下式(8)的三苯甲氧基 - 乙酸乙酯的步骤: 使式(8)化合物与乙基卤化镁反应制备下式(9)的1-三苯甲基氧基甲基 - 环丙醇:将式(9)的1-三苯甲氧基甲基 - 环丙醇与二异丙基溴甲基膦酸酯在溶剂中,在 用于制备下式(10)的(1-三苯甲基氧基甲基 - 环丙氧基甲基) - 膦酸二异丙酯的碱:固体形式,并将式(10)化合物的三苯甲基转化为羟基。

    Process for preparing beta-ketoester compound
    4.
    发明授权
    Process for preparing beta-ketoester compound 有权
    β-酮酯化合物的制备方法

    公开(公告)号:US06987199B2

    公开(公告)日:2006-01-17

    申请号:US10492092

    申请日:2002-10-14

    摘要: The present invention relates to a new process for preparing beta-ketoester compound of the following formula (1), which is a useful intermediate for the synthesis of such quinoline antibiotics as Ciprofloxacin, Levofloxacin, Gemifloxacin, Trovafloxacin, etc. The quinoline antibiotics obtained from the above compound of formula (1) show potent antibacterial activity, and so are advantageously used as a therapeutic agent for bacterial infections of humans or animals.

    摘要翻译: 本发明涉及一种制备下式(1)的β-酮酯化合物的新方法,它是合成喹诺酮类,左氧氟沙星,吉米沙星,曲伐沙星等喹啉类抗生素的有用中间体。 上述式(1)化合物显示出有效的抗菌活性,因此有利地用作人或动物细菌感染的治疗剂。

    Process for preparing acid salts of Gemifloxacin
    5.
    发明授权
    Process for preparing acid salts of Gemifloxacin 有权
    制备吉米沙星酸盐的方法

    公开(公告)号:US07361762B2

    公开(公告)日:2008-04-22

    申请号:US10510514

    申请日:2003-04-04

    IPC分类号: C07D221/02

    CPC分类号: C07D471/04

    摘要: The present invention relates to a process for preparing acid salts of Gemifloxacin, a quinolone type antibiotic agent having potent antimicrobial activity. The process according to the present invention can provide advantages such as simplicity of process, improvement of productivity and improvement of yield, and the like by reducing conventional three-step process to two-step process.

    摘要翻译: 本发明涉及一种制备具有强效抗菌活性的喹诺酮类抗生素的酸盐的方法。 根据本发明的方法可以通过将常规的三步骤过程减少到两步法来提供诸如方法的简单性,生产率的提高和产率的提高等的优点。

    Process for preparing acid salts of gemifloxacin
    6.
    发明申请
    Process for preparing acid salts of gemifloxacin 有权
    吉米沙星酸盐的制备方法

    公开(公告)号:US20050148622A1

    公开(公告)日:2005-07-07

    申请号:US10510514

    申请日:2003-04-04

    CPC分类号: C07D471/04

    摘要: The present invention relates to a process for preparing acid salts of Gemifloxacin, a quinolone type antibiotic agent having potent antimicrobial activity. The process according to the present invention can provide advantages such as simplicity of process, improvement of productivity and improvement of yield, and the like by reducing conventional three-step process to two-step process.

    摘要翻译: 本发明涉及一种制备具有强效抗菌活性的喹诺酮类抗生素的酸盐的方法。 根据本发明的方法可以通过将常规的三步骤过程减少到两步法来提供诸如方法的简单性,生产率的提高和产率的提高等的优点。