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    Preparation of intermediates useful in the synthesis of quinoline antibiotics
    5.
    发明授权
    Preparation of intermediates useful in the synthesis of quinoline antibiotics 失效
    制备可用于合成喹啉抗生素的中间体

    公开(公告)号：US6057455A

    公开(公告)日：2000-05-02

    申请号：US888519

    申请日：1997-07-07

    申请人： Joel M. Hawkins

    发明人： Joel M. Hawkins

    IPC分类号： C07D209/52 ,  C07C211/00

    CPC分类号： C07D209/52

    摘要： A process for preparing a compound of the formula ##STR1## wherein R.sup.1, m, o and p are described below, which comprises adding a base of the formula ##STR2## wherein R.sup.2, R.sup.3 and R.sup.4 are as described below, to a solution comprising a compound of the formula ##STR3## wherein R.sup.1, m, o and p are as described below, and a halonitromethane of the formula O.sub.2 NCH.sub.2 X, wherein X is a halogen atom dissolved in a non-aqueous inert solvent. The compounds of formula III are useful as intermediates in the syntheses of azabicyclo quinoline carboxylic acids, and their pharmaceutically acceptable salts and prodrugs, having antibacterial activity. This invention also relates to the base of formula IV wherein each R.sup.2 is butyl, R.sup.3 is hydrogen and each R.sup.4 is t-butyl.

    摘要翻译： 一种制备下式化合物的方法，其中R1，m，o和p如下所述，其包括将下式的其中R 2，R 3和R 4如下所述的下式加入到包含下式化合物的溶液中： R1，m，o和p如下所述，和式O 2 NCH 2 X的卤代硝基甲烷，其中X是溶解在非水惰性溶剂中的卤素原子。 式III化合物可用作合成具有抗菌活性的氮杂双环喹啉羧酸及其药学上可接受的盐和前药的中间体。 本发明还涉及式IV的碱，其中每个R 2是丁基，R 3是氢，每个R 4是叔丁基。

    Intermediates useful in the synthesis of quinoline antibiotics
    8.
    发明授权
    Intermediates useful in the synthesis of quinoline antibiotics 失效
    适用于合成喹啉类抗生素的中间体

    公开(公告)号：US06198000B1

    公开(公告)日：2001-03-06

    申请号：US09400396

    申请日：1999-09-21

    申请人： Joel M. Hawkins

    发明人： Joel M. Hawkins

    IPC分类号： C07C21163

    CPC分类号： C07D209/52

    摘要： A process for preparing a compound of the formula wherein R1, m, o and p are described below, which comprises adding a base of the formula wherein R2, R3 and R4 are as described below, to a solution comprising a compound of the formula wherein R1, m, o and p are as described below, and a halonitromethane of the formula O2NCH2X, wherein X is a halogen atom dissolved in a non-aqueous inert solvent. The compounds of formula III are useful as intermediates in the syntheses of azabicyclo quinoline carboxylic acids, and their pharmaceutically acceptable salts and prodrugs, having antibacterial activity. This invention also relates to the base of formula IV wherein each R2 is butyl, R3 is hydrogen and each R4 is t-butyl.

    摘要翻译： 下文描述了制备化学式R 1，m，o和p的化合物的方法，其包括将如下所述的式 ，o和p如下所述，和式O 2 NCH 2 X的卤代硝基甲烷，其中X是溶解在非水惰性溶剂中的卤素原子。 式III化合物可用作合成具有抗菌活性的氮杂双环喹啉羧酸及其药学上可接受的盐和前药的中间体。 本发明还涉及式IV的碱，其中每个R 2是丁基，R 3是氢，每个R 4是叔丁基。