CAS: 404844-11-7; 4-(Chloromethyl)-N-(4-Methyl-3-((4-(Pyridin-3-yl)Pyrimidin-2-yl)Amino)Phenyl)Benzamide

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CAS号1642-81-5 4-氯甲基苯甲酸 | CAS号152460-10-1 N-(5-氨基-2-甲基苯基)... | CAS号152460-09-8 N-(2-甲基-5-硝基苯基)... | CAS号99-55-8 2-氨基-4-硝基甲苯 | CAS号350-03-8 3-乙酰吡啶 | CAS号55314-16-4 1-(3-吡啶基)-3-(二甲... | CAS号66521-66-2 4-(3-吡啶基)-2-嘧啶胺 | CAS号1692-25-7 吡啶-3-硼酸 | CAS号99-99-0 对硝基甲苯 | CAS号7745-93-9 2-溴-4-硝基甲苯 | CAS号152459-95-5 伊马替尼

📜4-羟甲基苯甲酸置于氯化亚砜,三乙胺体系中,用 四氢呋喃,二氯甲烷 作为反应溶剂,化学反应 8.34H,反应生成 4-氯甲基-N-[4-甲基-3-[[4-(吡啶-3-基)嘧啶-2-基]氨基]苯基]苯甲酰胺
参考文献:伊马替尼碱的简便全合成及其类似物
标题:伊马替尼碱的简便全合成及其类似物
摘要:伊马替尼及其类似物通过改进的方法成功地合成了六个主要步骤,总收率为19.5-46.2%.嘧啶胺是通过烯胺酮和硝酸胍的反应制备的,无需使用有毒的氰胺.ñ-(2-甲基-5-硝基苯基)-4-(吡啶-3-基)嘧啶-2-胺,制备由铜催化的关键中间体为伊马替尼的合成ñ产率为82%的杂芳基胺-Arylation .在此c-N键形成反应中,使用铜盐代替了昂贵的钯化合物.使用水作作为反应溶剂,通过n 2 H 4 .H2O / Fecl 3 / C体系将中间体硝基化合物还原.
DOI:10.1021/op700270N

专利信息

专利号:WO-2013035102-A1
优先权日:2011-09-05
标 题 :Processes for the preparation of imatinib base and intermediates thereof
发明人：KOMPELLA AMALA KISHAN; RACHAKONDA SREENIVAS; GAMPA VENU GOPALA KRISHNA; ADIBHATLA KALI SATYA BHUJANGA RAO; NANNAPANENI VENKAIAH CHOWDARY
权利人:NATCO PHARMA LTD; KOMPELLA AMALA KISHAN; RACHAKONDA SREENIVAS; GAMPA VENU GOPALA KRISHNA; ADIBHATLA KALI SATYA BHUJANGA RAO; NANNAPANENI VENKAIAH CHOWDARY
摘要:The invention relates to an improved process for the preparation of highly pure imatinib base (99.99% HPLC purity) of formula (I) and the pharmaceutically acceptable acid addition salts thereof. This invention also relates to processes for the preparation of the intermediates in the synthesis of imatinib base.

专利号:WO-2012022217-A1
优先权日:2010-08-20
标 题 :N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)phenyl]benzamide derivatives, a preparation method and use for synthesis of imatinib thereof

专利号:US-2008187575-A1
优先权日:2004-08-27
标题:Pyrimidine Derivatives
发明人：KLEBL BERT; BAUMANN MATTHIAS; HOPPE EDMUND; BREHMER DIRK; DAUB HENRIK; KERI GYORGY; VARGA ZOLTAN; MAROSFALVI JENO; ORFI LASZLO
权利人:KLEBL BERT; BAUMANN MATTHIAS; HOPPE EDMUND; BREHMER DIRK; DAUB HENRIK; KERI GYORGY; VARGA ZOLTAN; MAROSFALVI JENO; ORFI LASZLO
摘要:The present invention relates to pyrimidine derivatives, methods for their synthesis, and the use of said pyrimidine derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferation disorders, cancer, leukemia, erectile dysfunction, cardiovascular diseases and disorders, inflammatory diseases, transplant rejection, immunological diseases, neuroimmunological diseases, autoimmune diseases, infective diseases including opportunistic infections, prion diseases and/or neuro-degeneration. Furthermore, the present invention relates to pharmaceutical compositions containing at least one pyrimidine derivative and/or pharmaceutically acceptable salts thereof as an active ingredient together with at least one pharmaceutically acceptable carrier, excipient or diluents as well as to methods for prophylaxis and/or treatment of the above-mentioned diseases and disorders.