NOVEL PROCESS FOR PURIFYING CEFOTIAM HYDROCHLORIDE
    53.
    发明申请
    NOVEL PROCESS FOR PURIFYING CEFOTIAM HYDROCHLORIDE 有权
    用于净化CEFOTIAM HYDROCHLORIDE的新工艺

    公开(公告)号:US20140011994A1

    公开(公告)日:2014-01-09

    申请号:US13997618

    申请日:2011-04-14

    申请人: Linggang Tao

    发明人: Linggang Tao

    IPC分类号: C07D501/12

    CPC分类号: C07D501/12 C07D501/36

    摘要: A method for treating cefotiam hydrochloride, comprises the following steps: step 1), dissolving the raw material cefotiam hydrochloride in water, treating it with an acidic salt, then cooling it, and filtering the precipitate to obtain an aqueous filtrate; step 2), adding a water-immiscible solvent to the above aqueous solution for extraction, and then separating the organic phase containing impurities to obtain an aqueous solution containing cefotiam hydrochloride; step 3) adding to the aqueous solution a poor solvent of cefotiam hydrochloride and controlling the temperature for recrystallization, washing the educed crystals by centrifugation, and drying them to obtain purified cefotiam hydrochloride. The cefotiam content of the refined cefotiam hydrochloride obtained by the method of the present invention is not less than 86%, the content of polymeric impurities is less than 0.3%, and the content of insoluble microparticles in the injection prepared therefrom is quite low.

    摘要翻译: 一种治疗头孢曲松盐酸盐的方法,包括以下步骤:步骤1)将原料盐酸头孢氨酸溶于水中,用酸性盐处理,然后冷却,过滤沉淀得到水性滤液; 步骤2),向上述水溶液中加入与水不混溶的溶剂萃取,然后分离含有杂质的有机相,得到含有头孢氨苄盐酸盐的水溶液; 步骤3)向水溶液中加入头孢氨苄盐酸盐的不良溶剂并控制重结晶温度,通过离心洗涤所得结晶,并干燥,得到纯化的盐酸头孢氨酸。 通过本发明方法得到的精制头孢他坦盐酸头孢氨肟含量不低于86%,聚合物杂质含量小于0.3%,并且由其制备的注射液中的不溶性微粒含量相当低。

    REFINING PROCESS OF CEFAMANDOLE SODIUM
    54.
    发明申请
    REFINING PROCESS OF CEFAMANDOLE SODIUM 有权
    CEFAMANDOLE SODIUM的精制工艺

    公开(公告)号:US20130303754A1

    公开(公告)日:2013-11-14

    申请号:US13885625

    申请日:2011-03-17

    申请人: Linggang Tao

    发明人: Linggang Tao

    IPC分类号: C07D501/58

    摘要: It discloses a novel process for refining cefamandole nafate, comprising: 1) adsorbing cefamandole nafate with strongly acidic ion exchange resin, followed by eluting the resin and collecting the eluate, to provide a primary purified cefamandole acid after concentration under reduced pressure; 2) neutralizing the primary purified cefamandole acid with an aqueous solution of sodium hydroxide or an aqueous solution of basic salt of sodium, followed by adjusting the pH value and filtrating out the insoluble substances with heating, thereby providing a secondary purified aqueous solution of cefamandole nafate; and 3) adding ethanol in a volume ratio between ethanol and water of 4:6 into the aqueous solution, to allow recrystallization under controlling the temperature, to provide a tertiary purified cefamandole nafate. The refined cefamandole nafate product has a purity of no less than 99.5%, mostly no less than 99.6%, with significantly low content of heavy metals.

    摘要翻译: 本发明公开了一种尖端头孢噻肟精制方法,其特征在于,包括:1)用强酸性离子交换树脂吸附头孢丹多头孢噻肟,然后洗脱树脂并收集洗脱液,减压浓缩后得到初级精氨酸头孢氨酸; 2)用氢氧化钠水溶液或钠盐水溶液中和初级纯化头孢氨肟酸,然后调节pH值,加热过滤除去不溶物质,从而提供头孢丹多头孢哌酮二次纯化水溶液 ; 和3)将乙醇与水的体积比为4:6的乙醇加入到水溶液中,以在控制温度下重结晶,得到叔纯化的头孢丹多头孢哌酮。 精制头孢丹多硝酸盐产品的纯度不低于99.5%,大部分不低于99.6%,重金属含量显着低。

    PURIFICATION METHOD OF AZTREONAM
    55.
    发明申请
    PURIFICATION METHOD OF AZTREONAM 有权
    AZTREONAM的纯化方法

    公开(公告)号:US20130296549A1

    公开(公告)日:2013-11-07

    申请号:US13885618

    申请日:2011-03-17

    申请人: Linggang Tao

    发明人: Linggang Tao

    IPC分类号: C07D417/12

    CPC分类号: C07D417/12 C07D501/36

    摘要: It discloses a process for refining Aztreonam, comprising the steps of 1) treating Aztreonam material with an alkali metal alkoxylate or an alkali earth metal alkoxylate under heating in the presence of a suitable solvent or a mixture of solvents, followed by adjusting the pH value with a suitable acid and cooling down to precipitate Aztreonam, which provides a primary purified Aztreonam; 2) adsorbing Aztreonam with strongly basic ion exchange resin, followed by eluting the resin and collecting the eluate, to provide a secondary purified Aztreonam after concentration under reduced pressure; 3) adjusting the pH value with a suitable acid to allow crystallization, followed by centrifuging and washing the resultant crystals, to provide a tertiary purified Aztreonam after drying. The refined Aztreonam product has a purity of no less than 99.2%, mostly no less than 99.5%, with little residue on ignition and significantly low content of heavy metals.

    摘要翻译: 它公开了一种精制氨曲南的方法,该方法包括以下步骤:1)在合适的溶剂或溶剂混合物的存在下,加热下用碱金属烷氧基化物或碱土金属烷氧基化物处理氨曲南,然后用 合适的酸并冷却沉淀阿斯曲南,其提供初级纯化的氨曲南; 2)用强碱性离子交换树脂吸附氨曲南,然后洗脱树脂并收集洗脱液,在减压浓缩后提供二次纯化的氨曲南; 3)用合适的酸调节pH值以使其结晶,然后离心分离和洗涤所得晶体,干燥后得到三级纯化的氨曲南。 精制的氨曲南产品的纯度不低于99.2%,大部分不低于99.5%,点燃残留少,重金属含量低。

    Cephalosporin compounds
    58.
    发明授权
    Cephalosporin compounds 失效
    CEPHALOSPORIN化合物

    公开(公告)号:US5202315A

    公开(公告)日:1993-04-13

    申请号:US494163

    申请日:1990-03-15

    CPC分类号: C07D501/36

    摘要: The present invention relates to new cephalosporin compounds of the formula(I), pharmaceutically acceptable non-toxic salts thereof, and physiologically hydrolyzable esters and solvates thereof, which have potent and broad antibacterial activities ##STR1## wherein R.sup.1 is a C.sub.1.about.4 alkyl, C.sub.3.about.4 alkenyl, C.sub.3.about.4 alkynyl group, or --C(R.sup.a)(R.sup.b)CO.sub.2 H.sub.1 wherein R.sup.a and R.sup.b are the same or different, and each is a hydrogen atom or a C.sub.1.about.4 alkyl group, or R.sup.a and R.sup.b form a C.sub.3.about.7 cycloalkyl group with the carbon atom to which they are linked;R.sup.2 is a C.sub.1.about.4 alkyl, C.sub.3.about.4 alkenyl or C.sub.3.about.4 cycloalkyl group, a substituted or unsubstituted amino group, or a substituted or unsubstituted phenyl group;R.sup.3 is hydrogen or a C.sub.1.about.4 alkyl group; andQ is N or CH.The invention further relates to a process for preparing said compounds, and to pharamaceutical compositions containing said compounds.

    Antibacterial cephalosporin compounds
    59.
    发明授权
    Antibacterial cephalosporin compounds 失效
    抗生素CEPHOROSPORIN化合物

    公开(公告)号:US5189157A

    公开(公告)日:1993-02-23

    申请号:US189936

    申请日:1988-05-03

    摘要: There are presented antibacterial cephalosporins having broad antimicrobial activity as well as intermediates for their formation, such compounds having the formula ##STR1## wherein X is ##STR2## R is hydrogen or a carboxylic acid protecting group; R.sub.1 is hydrogen or an acyl group;R.sub.2 is hydrogen or lower alkoxy; andR.sub.3 is carbocyclic aryl or alkyl carbocyclic aryl substituted on the ring with two or more of hydroxy and/or lower alkanoyl ester groups, with halogen being an optional additional ring substituent;as well as the corresponding readily hydrolyzable esters, pharmaceutically acceptable salts and hydrates of these compounds where R is hydrogen.

    摘要翻译: 呈现具有广谱抗微生物活性的抗菌头孢菌素及其形成中间体,具有下式的化合物,其中X为氢或羧酸保护基; R1是氢或酰基; R2是氢或低级烷氧基; 并且R 3是在具有两个或多个羟基和/或低级烷酰基酯基团的环上被取代的碳环芳基或烷基碳环基,其中卤素是任选的另外的环取代基; 以及其中R是氢的这些化合物的相应的易水解的酯,药学上可接受的盐和水合物。