📜1-(3-氯丙基)-4-甲氧基苯置于n-甲基吡咯烷酮,盐酸,对甲苯磺酸,三乙胺,肼体系中,用 1,4-二氧六环,二苯醚,乙醇,乙二醇甲醚 用作溶剂,化学反应 110.5H,反应生成2-(2-呋喃基)-7-[3-(4-甲氧基苯基)丙基]-7H-吡唑并[4,3-E][1,2,4]噻唑并[1,5-C]嘧啶-5-胺 参考文献:Design,Radiosynthesis,And Biodistribution Of A New Potent And Selective Ligand For In Vivo Imaging Of The Adenosine A2A Receptor System Using Positron Emission Tomography 标题:Design,Radiosynthesis,And Biodistribution Of A New Potent And Selective Ligand For In Vivo Imaging Of The Adenosine A2A Receptor System Using Positron Emission Tomography 摘要: Doi:10.1021/jm0009843
专利号:WO-2012127472-A1 优先权日:2011-03-22 标题:Process and intermediates for the preparation of preladenant and related compounds 发明人:MAROM EHUD; MIZHIRITSKII MICHAEL; RUBNOV SHAI 权利人:MAPI PHARMA LTD; MAROM EHUD; MIZHIRITSKII MICHAEL; RUBNOV SHAI 摘要:The present invention describes processes for the synthesis of 2-(furan-2-yl)-7-[2-[4-[4-(2-methoxyethoxy)phenyl]piperazin-l-yl] ethyl]-7H-pyrazolo[ 4,3-e ][1,2,4]- triazolo[1,5c] pyrimidin-5-amine (Preladenant) represented by the structure of formula (1 ), and solvates and salts thereof, especially salts with pharmaceutically acceptable acids. The process of the present invention is useful not only for Preladenant production, but also for the preparation of other biologically active compounds of general formula (17), such as A2a receptor antagonists used for the treatment of central nervous system diseases, among others. The present invention further relates to certain intermediates formed in such processes.
专利号:US-2023271983-A1 优先权日:2020-07-29 标题 :Functionalized isonitriles and products, preparation and uses thereof 发明人:SOTELO PÉREZ EDDY; AZUAJE GUERRERO JHONNY ALBERTO; MAJELLARO MARIA 权利人:UNIV SANTIAGO COMPOSTELA 摘要:The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.
1: Kang X, Yu J, Wei Y, Zhao P. The effect of A 2A receptor antagonist (SCH 442416) on the mRNA expression of Kir 2.1 and Kir 4.1 channels in rat retinal Müller cells under hypoxic conditions in vitro. Adv Clin Exp Med. 2013 Nov-Dec;22(6):825-9. 3: Yu J, Zhong Y, Shen X, Cheng Y, Qi J, Wang J. In vitro effect of adenosine A2A receptor antagonist SCH 442416 on the expression of glutamine synthetase and glutamate aspartate transporter in rat retinal Müller cells at elevated hydrostatic pressure. Oncol Rep. 2012 Mar;27(3):748-52. doi: 10.3892/or.2011.1565.
合成参考文献
参考文献:10.1007/s11302-006-9027-x 摘要:Cacciari B, Bolcato C, Spalluto G, Klotz K, Bacilieri M, Deflorian F, Moro S. Pyrazolo-triazolo-pyrimidines as adenosine receptor antagonists: A complete structure–activity profile. Purinergic Signalling. 2006 Nov 14;3(3):183–93. doi: 10.1007/s11302-006-9027-x. 参考文献:10.1007/s11302-009-9175-x 摘要:1st UK Purine Symposium: 19th November 2009. Purinergic Signal. 2010 Mar;6(1):125–44.