专利号:WO-2022256490-A9 优先权日:2021-06-03 标题:Improved synthesis of phosphoramidates for the treatment of hepatitis b virus 发明人:LOCKWOOD MARK 权利人:ANTIOS THERAPEUTICS INC 摘要:The synthesis of phosphoramidate prodrugs useful in the treatment of viral infections is disclosed. Specifically, an improved synthesis of phosphoramidate nucleotides useful in the treatment of Hepatitis B virus is disclosed.
专利号:US-2025179012-A1 优先权日:2022-03-04 标 题:Synthesis of sulfur(vi) compounds and reagents for same 发明人:LOPCHUK JUSTIN MATTHEW; SHULTZ ZACHARY 权利人:H LEE MOFFITT CANCER CT & RES 摘要:This disclosure provides reagents and processes for the synthesis of organic compounds, more particularly reagents and processes for the asymmetric synthesis of sulfur (VI) containing organic compounds.
专利号:US-2023287032-A1 优先权日:2020-08-14 标 题:Synthesis of fluorinated nucleotides 发明人:CHUNG CHEOL KEUN; LIU ZHIJIAN; MALIGRES PETER E; MAO EDNA; OBLIGACION JENNIFER V; PHILLIPS ERIC M; PIRNOT MICHAEL; POIRIER MARC; SONG ZHIGUO JAKE; WANG TAO 权利人:CHUNG CHEOL KEUN; LIU ZHIJIAN; MALIGRES PETER E; MAO EDNA; OBLIGACION JENNIFER V; PHILLIPS ERIC M; PIRNOT MICHAEL; POIRIER MARC; SONG ZHIGUO JAKE; WANG TAO; MERCK SHARP & DOHME LLC 摘要:The present invention relates to efficient processes useful in the preparation of fluorinated nucleosides, such as (O—{[(2R,3R,4S,5R)-5-(6-amino-9H-purin-9-yl)-4-fluoro-3-hydroxyoxolan-2-yl]methyl}O,O-dihydrogen phosphorothioate, also known as 2′-(S)-fluoro-thio-adenosine monophosphate or 2′-F-thio-AMP. 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.
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-10005807-B2 优先权日:2013-04-12 标题 :Synthesis of sialylated/fucosylated human milk oligosaccharides 发明人:CHASSAGNE PIERRE; KHANZHIN NIKOLAY; HEDEROS MARKUS JONDELIUS; CHAMPION ELISE; MATWIEJUK MARTIN; DEKANY GYULA 权利人:GLYCOM AS 摘要:An achemo-enzymatic synthesis of oligosaccharides of formula 1 is presented wherein R is selected from —OH, —N 3 and —OR 6 wherein R 6 is selected from allyl optionally substituted by one or more methyl, propargyl optionally substituted by one or more methyl, 2-trimethylsilyl-ethyl, —(CH 2) n —NH 2 and —(CH 2) n —N 3 wherein integer n is to 10, preferably 2 or 3, R is selected from sialyl moiety, —SO 3 H and —CH(R)—COOH wherein R is selected from H, alkyl and benzyl, R 2 is selected from H and fucosyl, R 3 is selected from H and sialyl, R 4 is selected from H and fucosyl, provided that at least one of R 3 and R 4 is H, and A is a divalent carbohydrate linker, having important biological activities and significant commercial value for the pharmaceutical and food industry.
专利号:US-12312325-B2 优先权日:2022-03-01 标 题:Methods and compounds useful in the synthesis of an AAK1 inhibitor 发明人:CHEN TAO; WU WENXUE; YAN JUN; ZENG XIANGLU; ZHAO MATTHEW MANGZHU 权利人:LEXICON PHARMACEUTICALS INC 摘要:Methods for the synthesis of (S)-1-((2′,6-bis(difluoromethyl)-[2,4′-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine and salts thereof are disclosed, as well as compounds useful therein.
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合成参考文献
参考文献:10.1021/ol201555z 摘要:Qian J, Liu Y, Zhu J, Jiang B, Xu Z. A novel synthesis of fluorinated pyrazoles via gold(I)-catalyzed tandem aminofluorination of alkynes in the presence of Selectfluor. Org Lett. 2011 Aug 19;13(16):4220–3. doi: 10.1021/ol201555z.