CAS: 125743-63-7; 4-((4-Methylpiperazin-1-yl)Methyl)Benzonitrile

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CAS号109-01-3 N-甲基哌嗪 | CAS号17201-43-3 α-溴对甲基苯甲腈 | CAS号69293-74-9 4-[(二乙基氨基)甲基]苯甲腈 | CAS号874-86-2 4-氰基苄氯 | CAS号104-85-8 对甲苯腈 | CAS号439691-80-2 4-(3-硝基苄基)吗啉 | CAS号515162-20-6 4-(4-甲基哌嗪-1-基)甲... | CAS号152459-95-5 伊马替尼 | CAS号125743-59-1 1-(4-((4-甲基哌嗪-1...

📜对甲苯腈置于n-溴代丁二酰亚胺(Nbs),过氧化苯甲酰体系中,用 氯仿 用作溶剂,化学反应 6.5H,反应生成伊马替尼合成中间体ⅰ
参考文献:A Facile Total Synthesis For Large-Scale Production Of Imatinib Base
标题:A Facile Total Synthesis For Large-Scale Production Of Imatinib Base
摘要:An Efficient,Economic Process Has Been Developed For The Production Of Imatinib With 99.99% Purity And 50% Overall Yield From Four Steps. Formation And Control Of All Possible Impurities Is Described. The Synthesis Comprises The Condensation Of N-(5-Amino-2-Methylphenyl)-4-(3-Pyridinyl)-2-Pyrimidineamine With 4-(4-Methylpiperazinomethyl)Benzoyl Chloride In Isopropyl Alcohol Solvent In The Presence Of Potassium Carbonate To Yield Imatinib Base.
Doi:10.1021/op300212U

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: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.