专利号:US-10597340-B2 优先权日:2013-05-10 标 题:Synthesis of fluorinated radiopharmaceuticals via electrochemical fluorination 发明人:SADEGHI SAMAN; HE QINGGANG; LEBEDEV ARTEM 权利人:UNIV CALIFORNIA 摘要:Provided herein are methods and compositions for the electrochemical selective radiofluorination of aromatic molecules. The resulting fluorine-18 labeled compounds are ideal radionuclides for use in Positron Emission Tomography (PET); they are also difficult to radiolabel efficiently and with high specific activity using existing approaches. For example, radiopharmaceuticals such as [F18]L-DOPA, which is indispensable in PET brain disease imaging, may be made electrochemically with high radiochemical yield and high specific activity using 18F-. The invention process described herein opens new possibilities and provides wider access to PET tracers such as 18F-L-Dopa, since 18F- is much more widely available than the 18F 2 , currently used for synthesis of electron rich substrates.
专利号:US-2011104055-A1 优先权日:2002-05-31 标题:Substituted n-aryl benzamides and related compounds for treatment of amyloid diseases and synucleinopathies 发明人:SNOW ALAN; WEIGELE MANFRED; LARSEN LESLEY; NGUYEN BETH; LAKE THOMAS; CASTILLO GERARDO; SANDERS VIRGINIA; WEAVERS REX T; LORIMER STEPHEN; LARSEN DAVID; COFFEN DAVID L; COFFEN CHARLOTTE 权利人:SNOW ALAN; WEIGELE MANFRED; LARSEN LESLEY; NGUYEN BETH; LAKE THOMAS; CASTILLO GERARDO; SANDERS VIRGINIA; WEAVERS REX T; LORIMER STEPHEN; LARSEN DAVID; COFFEN DAVID L; COFFEN CHARLOTTE 摘要:Compounds and their pharmaceutically acceptable salts, their synthesis and labeling, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, including Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment are provided. Also provided is the use of the disclosed compounds as imaging agents and methods for in vivo imaging and detection of amyloid and synuclein.
专利号:US-5047592-A 优先权日:1989-08-21 标题 :Selective hydrogenolysis process 发明人:CARPENTER JOEL F 权利人:ETHYL CORP 摘要:A relatively simple, economical process for the synthesis of epinine and related compounds is described. The process involves subjecting adrenalone, epinephrine or their respective congeners to selective hydrogenolysis using hydrogen and a metal hydrogenolysis catalyst such as palladium, platinum, rhodium or nickel. Preferably the reaction is conducted in a non-oxidizing acidic liquid reaction medium, such as in aqueous hydrochloric acid.
专利号:US-2016137567-A1 优先权日:2013-05-10 标题 :Synthesis of fluorinated radiopharmaceuticals via electrochemical fluorination
专利号:RU-2114852-C1 优先权日:1991-12-12 标题 :Cephem syn-isomer derivatives, method of their synthesis and pharmaceutical composition based on thereof
摘要:Herter, S.; Turner, N. J., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 3, 82. 参考文献:10.1007/bf00114628 摘要:Marr J, Kremer S, Sterner O, Anke H. Transformation and mineralization of halophenols by Penicillium simplicissimum SK9117. Biodegradation. 1996 Apr;7(2):165–71. doi: 10.1007/bf00114628. 参考文献:10.1007/s00253-014-5826-0 摘要:Fischer K, Majewsky M. Cometabolic degradation of organic wastewater micropollutants by activated sludge and sludge-inherent microorganisms. Applied Microbiology and Biotechnology. 2014 May 28;98(15):6583–97. doi: 10.1007/s00253-014-5826-0. 参考文献:10.1007/s10532-019-09885-8 摘要:Zhao ZQ, Zheng TC, Zhang WJ, Shen XL, Lv L, Li YM. Degradation of 3-fluoroanilne by Rhizobium sp. JF-3. Biodegradation. 2019 Dec;30(5-6):433–45. doi: 10.1007/s10532-019-09885-8. 参考文献:10.1016/j.femsle.2004.06.052|10.1111/j.1574-6968.2004.tb09717.x 摘要:Boersma FG, McRoberts WC, Cobb SL, Murphy CD. A 19F NMR study of fluorobenzoate biodegradation by Sphingomonas sp. HB-1. FEMS Microbiol Lett. 2004 Aug 15;237(2):355–61. doi: 10.1016/j.femsle.2004.06.052.