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
参考文献:10.1007/s12247-024-09813-1 摘要:Kritikos A, Singh R, Tsilomelekis G, Muzzio FJ. A Novel CFD Model of SMX Static Mixer Used in Advanced Continuous Manufacturing of Active Pharmaceutical Ingredients (API). J Pharm Innov. 2024 Mar 23;19(2). doi: 10.1007/s12247-024-09813-1.