专利号:US-2023174567-A1 优先权日:2020-05-22 标题:Synthesis of fluorinated nucleotides 发明人:ARMIGER TRAVIS; BELYK KEVIN M; BENKOVICS TAMAS; CHUNG CHEOL K; JI CHEN YINING; JOHNSON HEATHER CLAIRE; KLAPARS ARTIS; LIU ZHIJIAN; LIU ZHUQING; MOORE JEFFREY C; NEEL ANDREW J; PENG FENG; RUMMELT STEPHAN M; SALEHI MARZUARANI NASTARAN; SHERRY BENJAMIN D; SONG ZHIGUO JAKE; TURNBULL BEN WILLIAM HULME; WANG LU; XU FENG 权利人:MERCK SHARP & DOHME LLC 摘要:The present invention relates to efficient processes useful in the preparation of fluorinated nucleosides, such as (2S,3R,4S,5R)-5-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)-3-fluoro-4-hydroxy-2-(mercaptomethyl)tetrahydrofuran-3-yl dihydrogen phosphate, also known as 3′-fluoro-thio-guanosine monophosphate or 3′-F-thio-GMP. Such fluorinated nucleosides may be useful as a biologically active compound and or as an intermediate for the synthesis of more complex biologically active compounds. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation. (I)
专利号:US-3989691-A 优先权日:1973-01-05 标 题 :Preparation of cinchona alkaloid intermediates 发明人:TAYLOR EDWARD C; MARTIN STEPHEN F 权利人:UNIV PRINCETON 摘要:4-[3-(3-vinyl-1-acetyl-4-piperidyl)-1-propenyl]-6-methoxyquinoline, the corresponding epoxide and related compounds, useful in the synthesis of Cinchona alkaloids, are prepared by introducing an ylid group in the 4-position of a suitably substituted quinoline and reacting this ylid with an N-acetyl-4-piperidineacetaldehyde.
专利号:US-10287265-B2 优先权日:2015-03-09 标 题 :Enantiomers of 8-hydroxyquinoline derivatives and the synthesis thereof 发明人:Puskás László; Kanizsai István; PILLOT THIERRY; GYURIS Márió; Szabó András; Takács Ferenc; Hackler László 权利人:AVIDIN CO LTD; SONEAS RES CO LTD; SYNAGING SAS 摘要:Our invention relates to novel enantiomer derivatives of 8-hydroxyquinoline derivatives with general formula (I) and (II) and the synthesis thereof and pharmaceutically acceptable salts and metal complexes thereof, and the medicinal and/or pharmaceutical compositions comprising these compounds. n n n n n n n n n n The essence of the subject matter of the invention relates to the fact that prior art discloses the biological effect and characteristics only of the racemic products, the novel enantiomer derivatives according to the invention appear in our application for the first. n The subject matter of the invention furthermore relates to a novel, stereoselective synthesis for the preparation of the novel enantiomer derivatives according to the invention. The novel medicinal and/or pharmaceutical compositions comprising these enantiomers are suitable for the treatment of the named diseases, and the enanatiomers are used for manufacture of these compositions. These applications for manufacture of the compositions are also the subject matters of the invention. The compounds according to the invention can be used preferably as cytoprotective, neuroprotective, cardioprotective, anxiolytic and antidepressant agent for treatment of neuropsychiatric and neurologic diseases and diseases in connections with transplantations and with ischemia and reperfusion injuries thereof, and inhibition of organ, advantageously skin graft rejection. According to our studies the R-enantiomer has either sole or high biological effect in some cases.
专利号:US-5900227-A 优先权日:1996-06-17 标题 :Multicyclic nitrone spin trapping compositions 发明人:JANZEN EDWARD G; SANKURATRI NAGARAJU 权利人:OKLAHOMA MED RES FOUND 摘要:Multicyclic nitrone spin trapping compounds capable of forming stable free radical spin adducts are provided as well as methods for their synthesis. The multicyclic nitrone spin trapping compounds can be reacted with a free radical, such as a hydroxy or hydroperoxy radical, in solution to form a spin adduct which is stable and readily detectable by electron paramagnetic resonance (EPR) spectroscopy. The multicyclic nitrone spin traps can be used to detect free radicals in a sample such as a biological system. In one embodiment, the spin trapping compound, 1,3,3-trimethyl-6-azabicyclo-[3.2.1]oct-6-ene-N-oxide ('TRAZON') is provided, as well as methods for the synthesis of TRAZON and of modified forms of TRAZON. TRAZON can react with a wide range of different free radicals in solution to form free radical spin adducts which are readily detectable by EPR.
专利号:US-2019330188-A1 优先权日:2015-03-09 标 题:Enantiomers of 8-hydroxyquinoline derivatives and the synthesis thereof
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