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    METHOD OF PREPARING NILOTINIB
    2.
    发明公开
    METHOD OF PREPARING NILOTINIB 审中-公开
    制备尼罗替丁的方法

    公开(公告)号：EP3305777A1

    公开(公告)日：2018-04-11

    申请号：EP15892905.9

    申请日：2015-05-26

    申请人： Asymchem Laboratories (Tianjin) Co., Ltd. ,  Asymchem Life Science (Tianjin) Co., Ltd ,  Tianjin Asymchem Pharmaceutical Co., Ltd ,  Asymchem Laboratories (Fuxin) Co., Ltd ,  Jilin Asymchem Laboratories Co., Ltd

    发明人： HONG, Hao ,  JAMES, Gage ,  LI, Jiuyuan ,  LI, Changfeng ,  HUANG, Gaochao

    IPC分类号： C07D401/14

    摘要： The disclosure provides a method for preparing nilotinib. The preparation method includes the following steps: performing an aminocarbonylation reaction on a compound A and 3-(4-methyl-1H-imidazole-1-yl)-5-(trifluoromethyl) aniline to obtain an amination product; and performing deprotection treatment of an R group on the amination product to obtain the nilotinib, wherein the compound A has a structure shown in formula I, and in formula I, an R group is selected from benzyl, -COCF 3 , -CHO or -CO 2 R', where an R' group is C 1 ∼C 10 alkyl, C 1 ∼C 3 alkoxy ethyl or C 7 ∼C 19 aralkyl. The preparation method is short in synthesis route and mild in reaction condition. Moreover, with adoption of a special raw material, the preparation method may improve a yield of the nilotinib and simultaneously reduce process cost.

    摘要翻译： 本公开提供了制备尼罗替尼的方法。 该制备方法包括以下步骤：对化合物A和3-（4-甲基-1H-咪唑-1-基）-5-（三氟甲基）苯胺进行氨基羰基化反应，得到胺化产物; 进行氨基化产物上R基的脱保护处理得到尼罗替尼，其中化合物A具有式I所示结构，式I中R基选自苄基，-COCF 3，-CHO或-CO 2 R '，其中R'基团为C1〜C10烷基，C1〜C3烷氧基乙基或C7〜C19芳烷基。 该制备方法合成路线短，反应条件温和。 而且，通过采用特殊的原料，该制备方法可以提高尼罗替尼的产量，同时降低加工成本。

    CONTINUOUS OZONATION REACTION DEVICE AND OPERATING METHOD THEREFOR
    5.
    发明公开
    CONTINUOUS OZONATION REACTION DEVICE AND OPERATING METHOD THEREFOR 审中-公开
    连续臭氧反应装置及其操作方法

    公开(公告)号：EP2832438A1

    公开(公告)日：2015-02-04

    申请号：EP12846807.1

    申请日：2012-08-03

    申请人： Asymchem Laboratories (Tianjin) Co., Ltd ,  Asymchem Life Science (Tianjin) Co., Ltd ,  Tianjin Asymchem Pharmaceutical Co., Ltd ,  Asymchem Laboratories (Fuxin) Co., Ltd ,  Jilin Asymchem Laboratories Co., Ltd

    发明人： HONG, Hao ,  TAO, Jian ,  CHEN, Furong

    IPC分类号： B01J8/06 ,  B01J19/24 ,  B01J10/00 ,  C02F1/78

    CPC分类号： B01J19/2425 ,  B01J4/001 ,  B01J8/065 ,  B01J8/067 ,  B01J10/00 ,  B01J19/30 ,  B01J19/305 ,  B01J19/32 ,  B01J2204/002 ,  B01J2208/00884 ,  B01J2219/00033 ,  B01J2219/00085 ,  B01J2219/24 ,  B01J2219/30408 ,  B01J2219/30433 ,  B01J2219/32408 ,  B01J2219/32441 ,  C01B13/10 ,  C02F1/78

    摘要： The invention discloses an ozonization continuous reaction device, comprising a raw material inlet, a raw material distributing device, one or plurality of single reaction tubes, a product outlet and an air vent. The first end of the raw material distributing device is communicated with the raw material inlet; the first end of one or plurality of single reaction tubes is communicated with the second end of the raw material distributing device; the product outlet is communicated with the second end of the single reaction tube; ozone is conveyed to the single reaction tube via the air vent. The ozonization continuous reaction device provided by the invention realizes the large-scale and continuous production of the ozonization reaction on the basis of guaranteeing security; as the single reaction tube is arranged, the ozone amount and the liquid raw material existing in the single reaction tube in unit time become fewer, the reaction security is greatly improved; in addition, the liquid raw material and the ozone are continuously fed into the reaction device, the exhaust gas and the products are continuously discharged from the reaction device, the accumulation of the ozone is prevented, the security is greatly guaranteed, and the production capacity also can be improved to a higher level.

    摘要翻译： 本发明公开了一种臭氧化连续反应装置，包括原料入口，原料分配装置，一个或多个单一反应管，产品出口和通气口。 原料分配装置的第一端与原料入口连通， 一个或多个单反应管的第一端与原料分配装置的第二端连通， 产品出口与单一反应管的第二端连通; 臭氧通过排气口输送到单个反应管。 本发明提供的臭氧化连续反应装置在保证安全的基础上实现了臭氧化反应的大规模连续生产， 由于设置单个反应管，单位时间内单个反应管中存在的臭氧量和液态原料变少，反应安全性大大提高; 此外，液体原料和臭氧被连续地供给到反应装置中，废气和产物被连续地从反应装置排出，防止了臭氧的积聚，极大地保证了安全性，并且生产能力 也可以提高到更高的水平。