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142 条记录 (耗时 0.03 秒)

    METHOD OF MAKING CEFQUINOME PARTICLES
    81.
    发明申请
    METHOD OF MAKING CEFQUINOME PARTICLES 审中-公开
    制备酚类颗粒的方法

    公开(公告)号：US20120122832A1

    公开(公告)日：2012-05-17

    申请号：US13384606

    申请日：2010-07-19

    申请人： Hans Peter Niedermann ,  Heiko Bothe

    发明人： Hans Peter Niedermann ,  Heiko Bothe

    IPC分类号： A61K31/546 ,  C07D501/02 ,  C07D501/60

    CPC分类号： C07D501/46 ,  A61K31/545 ,  Y10T428/2982

    摘要： Disclosed is a process for the production of particles of a cefquinome acid addition salt, preferably cefquinome sulfate particles, by precipitation of cefquinome acid addition salt, preferably the sulfate, from a cefquinome betaine solution, wherein acid, preferably sulfuric acid, is added to the betaine solution. According to the invention the acid, preferably sulfuric acid, is added quickly in a single shot, in a molar excess of 40% to less than 100%. As a result, particles are formed that comprise agglomerates of microscale primary crystalline particles. This enables providing particles of cefquinome acid addition salt, preferably cefquinome sulfate, in particle sizes commensurate with micronized material, but with improved stability.

    摘要翻译： 公开了一种通过从头孢喹诺甜菜碱溶液中沉淀头孢氨酸加成盐（优选硫酸盐）来制备头孢奎宁酸加成盐，优选头孢氨酸硫酸盐颗粒的方法，其中将酸，优选硫酸加入到 甜菜碱溶液。 根据本发明，酸，优选硫酸以单次喷射快速加入，摩尔过量为40％至小于100％。 结果，形成包含微米级初级结晶颗粒的附聚物的颗粒。 这使得能够提供与微粉化材料相当的颗粒尺寸但具有改进的稳定性的头孢奎尼酸加成盐，优选头孢奎因硫酸盐颗粒。

    Cefazolin sodium pentahydrate crystal and its molecular assembly preparation method
    82.
    发明授权
    Cefazolin sodium pentahydrate crystal and its molecular assembly preparation method 有权
    头孢唑啉五水合物晶体及其分子装配制备方法

    公开(公告)号：US08178521B2

    公开(公告)日：2012-05-15

    申请号：US12085110

    申请日：2006-09-15

    申请人： Jingkang Wang ,  Yuxin Qian ,  Meijing Zhang ,  Jiehua Wu ,  Zhan'ao Yang

    发明人： Jingkang Wang ,  Yuxin Qian ,  Meijing Zhang ,  Jiehua Wu ,  Zhan'ao Yang

    IPC分类号： C07D501/36 ,  C07D501/02 ,  C07D501/12 ,  C07D501/59 ,  A61K31/545

    CPC分类号： C07D501/36 ,  C07D501/02 ,  C07D501/12

    摘要： The present invention relates to cefazolin sodium pentahydrate crystal and a method for assembly and preparation of the crystal molecule. The cefazolin sodium pentahydrate crystal molecule contains five water molecules, orthorhombic system, space group of C222(1), in which sodium ion is bonded to the cefazolin molecule with a coordinate bond. The method for assembly and preparation of cefazolin sodium pentahydrate crystal molecule are: adding a solvent to a reactor equipped with a jacket, adding cefazolin acid and a sodium salt, heating until the reaction solution is clear, stirring continuously, adjusting pH, upon the completion of the reaction, transferring the liquid into a jacketed crystallizer, adding crystal seeds or nucleating spontaneously, controlling cooling, slowly adding a antisolvent. The particle size of cefazolin sodium pentahydrate crystal according to the present invention is adjustable, and the distribution of particle size is concentrated, the product has good flowability, smooth surface, high crystallinity, good stability, and rapid dissolving rate.

    摘要翻译： 本发明涉及头孢唑啉五水合物晶体及其制备方法。 头孢唑啉五水合物晶体分子含有五个水分子，斜方晶系，C222（1）的空间基团，其中钠离子与头孢唑啉分子键合。 头孢唑啉五水合物晶体分子的组装和制备方法是：向装有夹套的反应器中加入溶剂，加入头孢唑啉酸和钠盐，加热至反应液澄清，连续搅拌，调整pH值，完成后 将液体转移到夹套结晶器中，加入晶种或自发成核，控制冷却，缓慢加入抗溶剂。 本发明头孢唑啉五水合物晶体的粒度可调，粒径分布浓缩，产品流动性好，表面光滑，结晶度高，稳定性好，溶解速度快。

    Crystalline β-lactam intermediate
    84.
    发明授权
    Crystalline β-lactam intermediate 有权
    结晶β-内酰胺中间体

    公开(公告)号：US06949641B2

    公开(公告)日：2005-09-27

    申请号：US10001544

    申请日：2001-10-31

    申请人： Julia Greil ,  Johannes Ludescher ,  Klaus Totschnig ,  Siegfried Wolf

    发明人： Julia Greil ,  Johannes Ludescher ,  Klaus Totschnig ,  Siegfried Wolf

    IPC分类号： C07D501/00 ,  C07D501/02 ,  C07D501/04 ,  C07D501/06 ,  C07D501/12 ,  C07D501/18 ,  C07D501/34

    CPC分类号： C07D501/00

    摘要： The novel intermediate compound crystalline 7-[2-(2-fomylaminothiazol-4-yl)-2 -(Z)-(methoxyimino)acetamido]-3-methoxymethyl-3-cephem-4-carboxylic acid-1 -(isopropoxy/crystallization of cefpodoxime proxetil. The crystallization process comprises dissolving or suspending the intermediate in the presence of a nitrile or a ketone or mixtures thereof; at a ratio of 1 gm of the intermediate to 2-15 ml nitrile; or at a ratio of 1 gm of the intermediate to 3-15 ml ketone; in the presence of 5-80 ml water; and thereafter isolating the intermediate in crystalline form and converting the intermediate by splitting off the formyl group from the amino group attached to the thiazolyl group, to obtain the desired product cefpodoxime proxetil, in the form of a diastereoisomeric mixture in a ratio of B/(A+B) of 0.5 to 0.6.

    摘要翻译： 新型中间体化合物结晶7- [2-（2-夫酰氨基噻唑-4-基）-2-（Z） - （甲氧基亚氨基）乙酰氨基] -3-甲氧基甲基-3-头孢烯-4-羧酸-1-（异丙氧基/ 结晶方法包括在腈或酮或其混合物的存在下将中间体溶解或悬浮;以1gm中间体与2-15ml腈的比例或以1g的比例 的中间体至3-15ml酮;在5-80ml水的存在下，然后分离出结晶形式的中间体，并通过从连接到噻唑基的氨基分离甲酰基转化中间体，得到 以B /（A + B）比为0.5至0.6的非对映异构体混合物形式的所需产品头孢泊肟酯。

    Process for producing cyclic compound
    85.
    发明申请
    Process for producing cyclic compound 有权
    环状化合物的制备方法

    公开(公告)号：US20050209450A1

    公开(公告)日：2005-09-22

    申请号：US10508659

    申请日：2003-03-26

    申请人： Akira Kaneko

    发明人： Akira Kaneko

    IPC分类号： C07D403/12 ,  C07D499/00 ,  C07D499/04 ,  C07D501/00 ,  C07D501/02 ,  C07D503/02 ,  C07D505/02 ,  C07D487/08

    CPC分类号： C07D403/12 ,  C07D499/00 ,  C07D501/00

    摘要： The present invention provides a method for preparing a β-lactam compound of the following Formula (3), which comprises the step of reacting a compound of the following Formula (1) with a trialkyl phosphite represented by the formula (R5O)3P (wherein R5 represents an ethyl group, etc.) in an amount of 2 to 5 moles per mole of the compound and the step of heating the resulting reaction mixture in a diluent, wherein said method is characterized by having the step of completely removing unreacted trialkyl phosphite from the reaction mixture prior to the step of heating. (wherein X represents S, etc., Y represents N, etc., n represents 0 or 1, R1 represents an optionally substituted alkyl group containing 1 to 10 carbon atoms, etc., R2 and R3 each represent an optionally substituted alkyl or heterocyclic group, etc., and R4 represents an alkenyloxy group containing 1 to 6 carbon atoms, etc., provided that R1 and R2 may together form a β-lactam ring, etc.)

    摘要翻译： 本发明提供了制备下式（3）的β-内酰胺化合物的方法，该方法包括下列步骤：使下式（1）的化合物与由式（R 5）表示的亚磷酸三烷基酯反应 O）3％P（其中R 5表示乙基等），每摩尔化合物为2至5摩尔，并且步骤 将所得反应混合物加热到稀释剂中，其中所述方法的特征在于具有在加热步骤之前从反应混合物中完全除去未反应的亚磷酸三烷基酯的步骤。 （其中X表示S等，Y表示N等，n表示0或1，R 1表示任选取代的含有1至10个碳原子的烷基等，R 0 > 2和R 3各自表示任选取代的烷基或杂环基等，R 4表示含有1至6个碳原子的链烯氧基， 等等，条件是R 1和R 2可以一起形成β-内酰胺环等）

    Process for preparation of 3-exomethylene cepham sulfoxide esters
    88.
    发明授权
    Process for preparation of 3-exomethylene cepham sulfoxide esters 失效
    3-亚甲基头孢烯亚砜酯的制备方法

    公开(公告)号：US5578721A

    公开(公告)日：1996-11-26

    申请号：US273309

    申请日：1994-07-11

    申请人： Niranjan L. Gupta ,  Ramanathan Sankaran ,  Shibu Varughese ,  Sakina Sitabkhan

    发明人： Niranjan L. Gupta ,  Ramanathan Sankaran ,  Shibu Varughese ,  Sakina Sitabkhan

    IPC分类号： C07D501/00 ,  C07D501/08 ,  C07D501/22 ,  C07D501/02

    CPC分类号： C07D501/00 ,  Y02P20/55

    摘要： A process for the manufacture of 3-exomethylene cepham sulfoxide ester of the formula ##STR1## wherein R is hydrogen, C.sub.1 -C.sub.3 alkyl, halomethyl, phenyl, substituted phenyl cyanomethyl, phenoxy, benzyloxy or substituted benzyl with a substituent group such as that selected from halo, alkyl, alkoxy, protected hydroxy, nitro, cyano and trifiuoromethyl, a group of the formula R.sub.2 --0-- wherein R.sub.2 is t-butyl, 2,2,2-trichloro ethyl, benzyl or substituted benzyl; a group of the formula R.sub.3 --[0].sub.n --CH.sub.2, wherein R.sub.3 is phenyl or substituted phenyl with the substituent group selected from halo, alkyl, alkoxy, protected hydroxy, nitro, cyano, or 1,4-cyclohexadienyl, and n is 0 or 1; or a substituted arylalkyl group of formula R.sub.4 --CH where R.sub.4 has the same meaning as R.sub.3 defined above and W is a protected hydroxy or protected amino group; and R.sub.1 is a carboxylic acid protecting group such as that selected from the group consisting of C.sub.1 -C.sub.4 alkyl, 2,2,2-trihalo alkyl, benzyl, substituted benzyl such as para nitrobenzyl, phenacyl, halo substituted phenacyl and benzhydryl is disclosed. Such compound is prepared by reacting a chlorosulfinylazetidinone of the formula ##STR2## wherein R and R.sub.1 have the same meanings as defined above, with a Lewis Acid type Friedel-Crafts catalyst and a sulfur compound in an inert solvent under anhydrous condition. These compounds find application as an intermediate for the preparation of cephalosporin antibiotics.

    摘要翻译： 其中R为氢，C 1 -C 3烷基，卤代甲基，苯基，取代的苯基氰基甲基，苯氧基，苄氧基或取代的苄基，其具有如下选择的取代基的制备式（I）的3-异亚甲基头孢烯亚砜酯的方法： 卤素，烷基，烷氧基，保护的羟基，硝基，氰基和三氟甲基，式R2-0-基团，其中R2是叔丁基，2,2,2-三氯乙基，苄基或取代的苄基; 式R 3 - [O] n -CH 2的基团，其中R 3是苯基或具有选自卤素，烷基，烷氧基，保护的羟基，硝基，氰基或1,4-环己二烯基的取代基的取代苯基，n是 0或1; 或式R4-CH的取代芳基烷基，其中R4具有与上述定义的R3相同的含义，W是受保护的羟基或被保护的氨基; 并且R 1是羧酸保护基，例如选自C 1 -C 4烷基，2,2,2-三卤代烷基，苄基，取代的苄基如对硝基苄基，苯甲酰甲基，卤素取代的苯甲酰甲基和二苯甲基的羧酸保护基。 通过在无水条件下，在惰性溶剂中使路易斯酸型Friedel-Crafts催化剂和硫化合物与式（VII）中R和R 1具有与上述定义相同的式的氯亚磺酰基氮杂环丁酮反应来制备该化合物。 这些化合物可用作制备头孢菌素抗生素的中间体。