CHEMICAL SYNTHESIS AND ANTI-TUMOR AND ANTI-METASTATIC EFFECTS OF DUAL FUNCTIONAL CONJUGATE
    42.
    发明申请
    CHEMICAL SYNTHESIS AND ANTI-TUMOR AND ANTI-METASTATIC EFFECTS OF DUAL FUNCTIONAL CONJUGATE 有权
    化学合成与抗肿瘤和双功能结合的抗分化作用

    公开(公告)号:US20130143826A1

    公开(公告)日:2013-06-06

    申请号:US13699869

    申请日:2011-05-27

    申请人: Gang Liu Nan Zhao Yao Ma

    发明人: Gang Liu Nan Zhao Yao Ma

    IPC分类号: C07K5/02

    摘要: The present invention discloses chemical synthesis, anti-tumor and anti-metastatic effects of a dual functional conjugate as shown by formula I. Specifically, paclitaxel or docetaxol is linked with muramyl dipeptide derivative to form a conjugate, thus dual anti-tumor and anti-metastatic effects are achieved by combination of chemotherapy and immunotherapy. The present invention also discloses that paclitaxel or docetaxol and muramyl dipeptide derivative conjugate is synthesized by combination of solid-phase and solution-phase synthesis, and said conjugate can be used in manufacture of anti-tumor medicaments as proved by reliable bioassays.

    摘要翻译: 本发明公开了如式I所示的双功能缀合物的化学合成,抗肿瘤和抗转移作用。具体地,紫杉醇或多西紫杉醇与胞壁酰二肽衍生物连接以形成缀合物,因此双重抗肿瘤和抗 - 通过化学疗法和免疫治疗联合实现转移效应。 本发明还公开了通过固相和溶液相合成的方法合成紫杉醇或多西他赛和胞壁酰二肽衍生物缀合物,并且所述缀合物可用于制造抗肿瘤药物,如通过可靠的生物测定证明的。

    Hole-jetting type mixer-reactor
    44.
    发明授权
    Hole-jetting type mixer-reactor 有权
    喷孔式混合反应器

    公开(公告)号:US08042988B2

    公开(公告)日:2011-10-25

    申请号:US11872982

    申请日:2007-10-16

    IPC分类号: B01F5/08

    摘要: A hole-jetting type mixer-reactor, comprises the following parts: a first feeding port, a second feeding port, an outer casing, an inner casing, jet holes and a mixing reaction zone. The inner casing is inside the outer casing, and the lower portion of the outer casing forms a buffer chamber with the inner casing. The first feeding port connects with the inner casing to constitute one flow channel, and the second feeding port connects with the buffer chamber to form the other flow channel. The jet holes are on the wall of the inner casing situated at lower portion of the buffer chamber. The mixing reaction zone is inside the inner casing below the jet holes. The cross section of the inner casing is rectangular or rectangle-like. The mixer-reactor can achieve a fast mixing of two reactant streams which reacts with instantaneous, complicated parallel or consecutive competing reactions. The time scale of the mixing process is several milliseconds.

    摘要翻译: 喷孔式混合反应器包括:第一进料口,第二进料口,外壳,内壳,喷射孔和混合反应区。 内壳在外壳内,外壳的下部形成有内壳的缓冲室。 第一进料口与内壳连接构成一个流动通道,第二进料口与缓冲室连接,形成另一流道。 喷射孔位于位于缓冲室下部的内壳的壁上。 混合反应区位于喷射孔下方的内壳内。 内壳的横截面为矩形或矩形。 混合器 - 反应器可以实现两种反应物流的快速混合,其与瞬时,复杂的平行或连续竞争反应反应。 混合过程的时间尺度为几毫秒。

    Process for Preparing Pemetrexed Disodium and Its Intermediate, 4-(4-Carbomethoxyphenyl) Butanal
    46.
    发明申请
    Process for Preparing Pemetrexed Disodium and Its Intermediate, 4-(4-Carbomethoxyphenyl) Butanal 失效
    制备培美曲塞二钠及其中间体4-(4-甲氧基苯基)丁醛的方法

    公开(公告)号:US20110124861A1

    公开(公告)日:2011-05-26

    申请号:US12995257

    申请日:2008-11-25

    申请人: Jinliang Li Nan Zhao

    发明人: Jinliang Li Nan Zhao

    IPC分类号: C07D487/04 C07C67/56

    摘要: The present invention provides a process for preparing pemetrexed disodium and its intermediate, 4-(4-carbomethoxyphenyl)butanal. The process for preparing the intermediate comprises the following steps: condensing methyl 4-bromobenzoate with 3-buten-1-ol; extracting with an organic solvent during the work-up; adding silica gel to decolorize; and evaporating the organic solvent to give 4-(4-carbomethoxyphenyl)butanal. The product obtained by the present process, with a yield of higher than 80%, and a purity measured by GC of higher than 95%, may be directly used in the next bromination reaction for synthesizing pemetrexed disodium without purification. The present process is suitable for industrial production, as the operation is simple and the reagents used are cheap and readily available.

    摘要翻译: 本发明提供了培美曲塞二钠及其中间体4-(4-甲酯基苯基)丁醛的制备方法。 制备中间体的方法包括以下步骤:将4-溴苯甲酸甲酯与3-丁烯-1-醇缩合; 在处理过程中用有机溶剂萃取; 加入硅胶脱色; 并蒸发有机溶剂,得到4-(4-甲酯基苯基)丁醛。 通过本方法得到的产物,产率高于80%,通过GC测定的纯度高于95%,可以直接用于下一次溴化反应,无需纯化即可合成培美曲塞二钠。 本方法适用于工业生产,操作简单,使用的试剂便宜且易于获得。