双(2-甲氧基乙基)胺置于正丁基锂体系中,用 乙醚,正己烷 用作溶剂,化学反应 3.5H,反应生成[双(2-甲氧基乙基)胺]三氟化硫 参考文献:Bis(2-Methoxyethyl)Aminosulfur Trifluoride: A New Broad-Spectrum Deoxofluorinating Agent With Enhanced Thermal Stability 标题:Bis(2-Methoxyethyl)Aminosulfur Trifluoride: A New Broad-Spectrum Deoxofluorinating Agent With Enhanced Thermal Stability 摘要:Bis(2-Methoxyethyl)Aminosulfur Trifluoride,(Ch3och2Ch2)(2)Nsf3 (Deoxo-Fluor Reagent),Is A New Deoxofluorinating Agent That Is Much More Thermally Stable Than Dast (C2H5)(2)Nsf3 And Its Congeners. It Is Effective For The Conversion Of Alcohols To Alkyl Fluorides,Aldehydes/ketones To The Corresponding Gem-Difluorides,And Carboxylic Acids To The Trifluoromethyl Derivatives With,In Some Cases,Superior Performance Compared To Dast. The Enhanced Stability Is Rationalized On The Basis Of Conformational Rigidity Imposed By A Coordination Of The Alkoxy Groups With The Electron-Deficient Sulfur Atom Of The Trifluoride. Doi:10.1021/jo990566+
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-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-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.
专利号:US-10173993-B2 优先权日:2015-12-09 标题 :Process for the synthesis of sulfones and sulfonamides 发明人:VON WOLFF NIKLAS; CHAR JOËLLE; CANTAT THIBAULT 权利人:COMMISSARIAT ENERGIE ATOMIQUE 摘要:A one pot single step process is described for the synthesis of a compound, including a labeled compound, containing a sulfonyl functional group comprising the step of mixing together a silane, an SO 2 source, an electrophilic compound, an activating compound and optionally a metal catalyst. A process for producing tracers from a labeled sulfonyl containing compound prepared by the described process is also included.
专利号:US-9982005-B2 优先权日:2013-04-04 标 题 :Macrolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.