2-氨基-4-硝基甲苯置于硝酸,Sodium Hydroxide体系中,用 乙醇,水 用作溶剂,化学反应 3.0H,反应生成2-甲基-5-硝基苯基胍 参考文献: Processes For Preparing Imatinib And Pharmaceutically Acceptable Salts Thereof[fr] Procédés De Préparation D'Imatinib Et De Ses Sels Pharmaceutiquement Acceptables 标题: Processes For Preparing Imatinib And Pharmaceutically Acceptable Salts Thereof[fr] Procédés De Préparation D'Imatinib Et De Ses Sels Pharmaceutiquement Acceptables 摘要:制备伊马替尼及其药用可接受的盐,特别是甲磺酸伊马替尼的工艺已被披露.
专利号:US-8334381-B2 优先权日:2006-11-16 标题 :Process for the preparation of intermediates useful in the synthesis of imatinib 发明人:FALCHI ALESSANDRO; GRENDELE ENNIO; MOTTERLE RICCARDO; STIVANELLO MARIANO 权利人:FALCHI ALESSANDRO; GRENDELE ENNIO; MOTTERLE RICCARDO; STIVANELLO MARIANO; ITALIANA SINT SPA 摘要:It is the object of the present invention a process for the preparation of 4-methyl-N3-[4-(3-pyridinyl)-2-pyrimidinyl]-1,3-benzenediamine and analogues thereof, intermediates useful for the synthesis of Imatinib, or 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide.
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:US-2011097268-A1 优先权日:2006-08-23 标 题 :Radiohaloimatinibs and methods of their synthesis and use in pet imaging of cancers 发明人:BORNMANN WILLIAM; ALAUDDIN MIAN; GELOVANI JURI; GHOSH PRADIP; GUO LIWEI; HAN DONGMEI; MAXWELL DAVID; MUKHOPADHYAY UDAY; PENG ZHENGHONG; SHAVRIN ALEKSANDR; YING YUNMING 权利人:UNIV TEXAS 摘要:We disclose methods of synthesizing radiohalidated organic compounds and their use in positron emission tomography (PET) imaging of cancer cells.
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-8609842-B2 优先权日:2010-04-23 标题 :Method for synthesizing Imatinib 发明人:SHEN XIN; HE XIAO; YANG JIDONG; WU SHAOHONG; ZHAN HUAXING 权利人:SHEN XIN; HE XIAO; YANG JIDONG; WU SHAOHONG; ZHAN HUAXING; FUJIAN SOUTH PHARMACEUTICAL CO LTD; SHANGHAI PARLING PHARMATECH CO LTD 摘要:In the present invention, a synthesis method of Imatinib is disclosed, which comprises the following steps: the Imatinib, namely 4-(4-methyl-piperazin-1-ylmethyl)-N-[4-methyl-3-[4-(3-pyridinyl)-pyrimidin-2-ylamino]-benzami de shown in formula (III), is formed by reacting 4-methyl-N-3-(4-pyridin-3-yl-pyrimidin-2-yl)-1,3-benzenediamine shown in formula (I) with 4-(4-methyl-piperazin-1-methyl)-benzoic ester shown in formula (II), under the action of a base and in a non-protonic organic solvent, n nin the above generic chemical structural formula, R represents aliphatic alkyl having 1-10 carbon, phenyl, substituted phenyl, benzyl or substituted benzyl. The present invention provides a new synthesis method of Imatinib, which is formed under mild reaction conditions, and is environmentally friendly with a high-yield.
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.