LINEZOLID INTERMEDIATE AND METHOD FOR SYNTHESIZING LINEZOLID
    2.
    发明申请
    LINEZOLID INTERMEDIATE AND METHOD FOR SYNTHESIZING LINEZOLID 有权
    LINEZOLID中间体和用于合成LINEZOLID的方法

    公开(公告)号:US20140024827A1

    公开(公告)日:2014-01-23

    申请号:US14008124

    申请日:2012-04-12

    摘要: Provided are a linezolid intermediate and the preparation method thereof and a method for synthesizing linezolid. The structure of the intermediate is shown as formula F2, wherein the compound is prepared by a condensation reaction of (S)—N—(3-chloro-2-hydroxy-1-propyl) acetamide and the compound shown in formula F4. In the preparation methods of the compound shown in formula F2 and linezolid, the reaction system is mild, side reactions are few and the product yield is high.

    摘要翻译: 提供了一种利奈唑胺中间体及其制备方法和合成利奈唑胺的方法。 中间体的结构如式F2所示,其中化合物通过(S)-N-(3-氯-2-羟基-1-丙基)乙酰胺与式F4所示的化合物的缩合反应制备。 在式F2和利奈唑胺的化合物的制备方法中,反应体系温和,副反应少,产物收率高。

    Dehydroxy vancomycin, the preparation, pharmaceutical composition and the use
    3.
    发明授权
    Dehydroxy vancomycin, the preparation, pharmaceutical composition and the use 有权
    脱羟万古霉素,制剂,药物组合物及用途

    公开(公告)号:US08338372B2

    公开(公告)日:2012-12-25

    申请号:US12680650

    申请日:2008-08-25

    摘要: The present invention provides a deshydroxy vancomycin compound,a method of its preparation and a pharmaceutical composition comprising a pharmaceutically effective amount of the deshydroxy vancomycin and the use of the said composition in the preparation of drugs for the treatment of susceptible bacteria infections. The method includes the following steps: (1) preparing a concentrated vancomycin solution containing the deshydroxy vancomycin by fermentations of Amycolatopsis Orientalis with Deposit No. CGMCCNO.1183; (2) separating and purifing the concentrated vancomycin solution to obtain a refined filtrate of vancomycin hydrochloride containing the deshydroxy vancomycin by column chromatography; and (3) further separating and purifing the refined filtrate to obtain the deshydroxy vancomycin by chromatography. Wherein, separation and purification is processed by column chromatography in a gel chromatography column containing a salt-water mobile phase, separation and purification is processed by chromatography in a macroporous adsorption resin chromatography column containing a buffer-methanol mobile phase.

    摘要翻译: 本发明提供了一种脱羟基万古霉素化合物,其制备方法和包含药学有效量的脱羟万古霉素的药物组合物,以及所述组合物在制备用于治疗易感细菌感染的药物中的用途。 该方法包括以下步骤:(1)通过发酵具有沉积物号CGMCCNO.1183的Amycolatopsis Orientalis的发酵制备含有脱羟万古霉素的浓缩万古霉素溶液; (2)分离纯化浓缩的万古霉素溶液,通过柱色谱法得到含有脱羟万古霉素的万古霉素盐酸盐精制滤液; 和(3)进一步分离和纯化精制滤液,通过色谱法获得脱羟万古霉素。 其中分离纯化在含有盐水流动相的凝胶色谱柱中通过柱色谱法处理,分离和纯化在含有缓冲液 - 甲醇流动相的大孔吸附树脂色谱柱中通过色谱法处理。

    Use of Cloud Point System in Biotransformation
    5.
    发明申请
    Use of Cloud Point System in Biotransformation 审中-公开
    使用云点系统进行生物转化

    公开(公告)号:US20070259428A1

    公开(公告)日:2007-11-08

    申请号:US10567439

    申请日:2004-07-05

    IPC分类号: C12N15/87

    CPC分类号: C12P33/02 C12N1/38

    摘要: The invention relates to the field of microbial technology. It discloses a method to apply the cloud point system (CPS) in biotransformation by selecting one or more types of nonionic surfactant to form a aqueous system with a cloud point below the microbial transformation temperature, which serves as transformation medium. The method disclosed is suitable in particular for microbial transformation of hydrophobic compounds, for the system where substrate or product inhibits microbial growth or where product is further degraded by microbes. The CPS in the present invention forms a microemulsion of water-in-oil and oil-in-water, where the drops of surfactant is able to solubilize, serving as substrate reservoir and product extractant. This enhances bioavailability of substrates and elimination of product inhibition. The large water vesicles existing in the continuous surfactant phase provide aqueous environment to the cells where they can be sheltered from detrimental effects of surfactants, resulting in improvement of biocompatibililty.

    摘要翻译: 本发明涉及微生物技术领域。 它公开了一种通过选择一种或多种类型的非离子表面活性剂来应用浊点系统(CPS)进行生物转化的方法,以形成低于微生物转化温度的浊点的水系,其作为转化介质。 所公开的方法特别适用于疏水化合物的微生物转化,其中底物或产物抑制微生物生长或其中产物被微生物进一步降解的系统。 本发明中的CPS形成了油包水和水包油的微乳液,其中表面活性剂的液滴能够溶解,作为底物贮存器和产物萃取剂。 这增强了底物的生物利用度和消除了产物的抑制作用。 存在于连续表面活性剂相中的大水泡为细胞提供水环境,在那里可以避免表面活性剂的不利影响,导致生物相容性的提高。

    Lycopene intermediate 1, 3, 6, 10-tetra-double bond pentadec-carbon phosphonate as well as preparation method and use thereof
    6.
    发明授权
    Lycopene intermediate 1, 3, 6, 10-tetra-double bond pentadec-carbon phosphonate as well as preparation method and use thereof 有权
    番茄红素中间体1,3,6,10-四 - 双十五碳酸膦酸酯及其制备方法和用途

    公开(公告)号:US08765988B2

    公开(公告)日:2014-07-01

    申请号:US13583635

    申请日:2011-03-09

    IPC分类号: C07F9/40

    CPC分类号: C07F9/4015

    摘要: The invention relates to a novel important lycopene intermediate 3,7,11-trimethyl-1,3,6,10-tetraene-dodecyl diethyl phosphonate. A current lycopene intermediate 2,4,6,10-tetra-double bond pentadec-carbon phosphonate is difficult to synthesize. The invention provides a novel intermediate, which has the following synthesis steps of: preparing 2,6,10-trimethyl-3,5,9-undecane triene-1-aldehyde from pseudoionone; preparing 2,6,10-trimethyl-2,5,9-undecane triene-1-aldehyde from the 2,6,10-trimethyl-3,5,9-undecane triene-1-aldehyde; and subjecting the 2,6,10-trimethyl-2,5,9-undecane triene-1-aldehyde and tetraethyl methylenediphosphonate to condensation reaction to obtain target product. The invention can generate novel intermediate from raw material pseudoionone only by four reactions, thus the reactions are easy to control and great industrial value are achieved.

    摘要翻译: 本发明涉及新型重要的番茄红素中间体3,7,11-三甲基-1,3,6,10-四烯十二烷基二乙基膦酸酯。 目前的番茄红素中间体2,4,6,10-四 - 双十五碳酸膦难以合成。 本发明提供了一种新的中间体,其具有以下合成步骤:由假雄酮制备2,6,10-三甲基-3,5,9-十一烷三烯-1-醛; 由2,6,10-三甲基-3,5,9-十一烷三烯-1-醛制备2,6,10-三甲基-2,5,9-十一烷三烯-1-醛; 并使2,6,10-三甲基-2,5,9-十一烷三烯-1-醛和四亚乙基二膦酸四乙酯进行缩合反应,得到目标产物。 本发明只能通过四个反应从原料假雄酮生成新的中间体,因此反应易于控制,实现了巨大的工业价值。

    2, 6-Dinitrogen-Containing Substituted Purine Derivatives, The Preparation And Uses Thereof
    8.
    发明申请
    2, 6-Dinitrogen-Containing Substituted Purine Derivatives, The Preparation And Uses Thereof 有权
    2,6-Dinitrogen-Containing替代嘌呤衍生物,其制备和用途

    公开(公告)号:US20100144663A1

    公开(公告)日:2010-06-10

    申请号:US12596669

    申请日:2008-04-17

    摘要: The present invention provides 2,6-dinitrogen-containing substituted purine compounds of formula (A) or salts or solvates thereof or the solvates of salts thereof, as well as pharmaceutical compositions containing such compounds. The compounds of the present invention have the characteristics of lower toxicity, broad anticancer spectrum, higher anticancer activity, good stability and the like. The compounds are useful for the manufacture of an antitumor medicament. The present invention also provides a process for preparing these compounds.

    摘要翻译: 本发明提供式(A)的2,6-二氮的取代嘌呤化合物或其盐或溶剂合物或其盐的溶剂化物,以及含有这些化合物的药物组合物。 本发明化合物具有毒性低,抗癌谱广,抗癌活性高,稳定性好等特点。 该化合物可用于制造抗肿瘤药物。 本发明还提供了制备这些化合物的方法。