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-6410643-B1 优先权日:2000-03-09 标题 :Solid phase synthesis method and reagent 发明人:SWANSON MELVIN J 权利人:SURMODICS INC 摘要:A reagent composition adapted to be coated onto a support surface in order to provide that surface with a high density of reactive groups. The surface, thus coated, can be used for any suitable purpose, and is particularly well suited for use as a solid phase synthesis support surface. The synthesis support surface, in turn, can be used in repetitive and combinatorial syntheses such as the synthesis of polynucleotides, polypeptides and polysaccharides. The polymeric coating can be used to provide increased effective surface area, particularly in situations in which the effective area of the support surface is itself limited, as on the surface of a silicon wafer. In so doing, the polymeric coating provides an optimal combination of such properties as reactive density and surface area or volume.
专利号:US-12122769-B2 优先权日:2017-10-19 标题 :Synthesis of antibacterial aminoglycoside analogs 发明人:TREND RAISSA; DAPPEN MICHAEL; HENRY CHRISTOPHER E; GOLDBLUM ADAM AARON; AGGEN JAMES BRADLEY; MENDONÇA RICARDO FILIPE DE JESUS GONÇALVES; SARDINHA JOÃO CARLOS FALCÃO 权利人:CIPLA USA INC 摘要:The present disclosure relates to novel methods for preparing antibacterial aminoglycoside compounds, as well as to related intermediates, and crystal forms thereof, useful in such methods.
专利号:AU-2022253019-A1 优先权日:2021-04-09 标题:Synthesis of rapamycin analog compounds
专利号:EP-3697797-A1 优先权日:2017-10-19 标题 :Synthesis of antibacterial aminoglycoside analogs
专利号:CN-111655709-A 优先权日:2017-10-19 标 题:Synthesis of Antibacterial Aminoglycoside Analogs
[参考文献]: Jesper Stergaard, Et Al. Determination Of Octanol-Water Partition Coefficients For Carbonate Esters And Other Small Organic Molecules By Microemulsion Electrokinetic Chromatography. Electrophoresis. 2003 Mar;24(6):1038-46.
合成参考文献
摘要:Zimmer, R.; Trawny, D., Science of Synthesis Knowledge Updates, (2013) 4, 161. 摘要:Ros, A.; Fernández, R.; Lassaletta, J. M., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 417.