CAS: 152460-10-1; N-(5-Amino-2-Methylphenyl)-4-(3-Pyridyl)-2-Pyrimidineamine

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CAS号404844-11-7 N-[4-甲基-3-(4-吡啶... | CAS号152459-95-5 伊马替尼

伊马替尼置于盐酸,溶剂黄146体系中,用97%的收率获得n-(5-氨基-2-甲基苯基)-4-(3-吡啶基)-2-氨基嘧啶
参考文献:伊马替尼可光活化笼状前药的设计,合成和表征
标题:伊马替尼可光活化笼状前药的设计,合成和表征
摘要:伊马替尼是第一种被批准用于临床的蛋白激酶抑制剂,并且是靶向治疗概念的开创性药物.在此,我们报道了伊马替尼可光活化的笼状前药的设计,合成,光动力学性质和体外酶促评价.这种方法可以对由紫外线触发的伊马替尼的激活进行空间和时间控制.光激活概念在这种重要的激酶抑制剂上的成功应用为笼养技术作为激酶领域的一种可行方法提供了进一步的证据.提出的可光活化的伊马替尼前药将作为药理学工具,用于更详细地研究伊马替尼对生物系统的影响将非常有用.
Doi:10.1002/cmdc.201500163

专利信息

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-2021033174-A1
优先权日:2020-10-31
标题 :Synthesis, characterization, and biological evaluation of ibuprofen derivative against colon and breast cancer cell-lines
发明人：AL-OBAIDI ZAID MAHDI JABER; AL-ANI AWATEF A IBRAHIM; SHAHEED DHURGHAM QASIM
权利人:AL OBAIDI ZAID MAHDI JABER; AL ANI AWATEF A IBRAHIM; SHAHEED DHURGHAM QASIM
摘要:The synthesis of novel conjugate of ibuprofen with the 6-methyl-N1-(4-(pyridin-3-yl) pyrimidin-2-yl) benzene-1,3-diamine derivative showed a potential antiproliferative activity against both colon cancer and breast cancer cell lines. The chemical structure was characterized and confirmed by spectral (FTIR,1H-NMR and 13C NMR), and the Differential Scanning Colorimetry (DSC) Thermal analyzer. While the biological activity was estimated by Genetic Optimization of Ligand Docking (GOLD) software supplied by Cambridge Crystallographic Data Centre (CCDC) and conducted in vitro with the MTT and the calculation of the IC50. The docking process was successfully performed and the chemical synthesis yield was reasonably high. The spectral interpretations show characteristic identification of the target chemical compound. The results indicated a powerful antitumor drug against breast cancer (MCF7) and colon (HCT116) cell lines. On the other hand, to evaluate the toxicity profile, the Madin-Darby Canine Kidney (MDCK) normal (noncancerous) cell line, was utilized.

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-2023098592-A1
优先权日:2021-11-30
标题:Preparation method for carbon-loaded iron-based catalyst and use thereof in synthesis of intermediates of anti-cancer inhibitors

专利号:US-2023065387-A1
优先权日:2019-10-14
标题:Synthesis of tyrosine kinase inhibitors

专利号:CN-114315595-B
优先权日:2021-11-30
标题 :Preparation method of a carbon-supported iron-based catalyst and its application in the synthesis of anti-cancer inhibitor intermediates