双苯磺酰亚胺置于sodium Hydroxide,Fluorine体系中,用 水,乙腈 用作溶剂,化学反应 0.33H,反应生成N-氟代双苯磺酰胺 参考文献:Comparative Studies On The Enantioselective Fluorination Of Oxindoles With Structurally Modified N-Fluorobenzenesulfonimides 标题:Comparative Studies On The Enantioselective Fluorination Of Oxindoles With Structurally Modified N-Fluorobenzenesulfonimides 摘要:Structurally Modified N-Fluorobenzenesulfonimides (Nfsis) Have Been Used To Study The Enantioselective Fluorination Of Oxindoles In The Presence Of A Bis-Cinchona Alkaloid,(Dhqd)(2)Phal,As The Catalyst. We Observe That The Nfsi Analogues Bearing Two Tert-Butyl Groups At The Para-Position Of The Symmetric Phenyl Rings Led To An Enhanced Enantioselectivity In Most Cases (Up To 96% Ee) Compared With The Unmodified Nesis (Less Than 69% Ee). (C) 2013 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Tet.2013.04.037
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:WO-2025101716-A1 优先权日:2023-11-07 标题:Processes for synthesis of trifunctionalized sulfur(vi) compounds 发明人:LOPCHUK JUSTIN; SHULTZ ZACHARY; ATHAWALE PARESH 权利人:H LEE MOFFITT CANCER CT & RES 摘要:This disclosure describes processes for the asymmetric synthesis of trifunctionalized sulfur(VI) containing organic compounds of Formula I and Formula VI, as well as compounds of Formula I and Formula VI prepared by the processes described.
专利号:US-12234203-B2 优先权日:2020-03-12 标 题:Process for the synthesis of cannabidiol and intermediates thereof 发明人:ANAND RADHIKA; SHARMA SUMIT; SINGH CHAM PANKAJ; GANNEDI VEERANJANEYULU; KUMAR MUKESH; PRATAP SINGH VARUN; PRAKASH RAHUL VISHAV; ASREY VISHWAKARMA RAM; PAL SINGH PARVINDER 权利人:COUNCIL OF SCIENT AND INDUSTRIAL RESEARCH AN INDIAN REGISTERED BODY INCORPORATED UNDER THE REGN OF T; COUNCIL OF SCIENT AND INDUSTRIAL RESEARCH AN INDIAN REGISTERED BODY INCORPORATED UNDER THE REGN OF S 摘要:The present invention relates to process for the preparation of cannabidiol (A) from the coupling of (D) and (E) through the intermediates (C) and (D) starting from compound (B). The invention further relates to the novel compounds (B), (C), (D) and (E) and reagents used in this process. More specifically, this invention provides the manufacturing of Cannabidiol (A) in milligram to gram or kilogram scale.
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.
[参考文献]: Toshiaki Suzuki, Et Al. Enantioselective Fluorination Of Tert-Butoxycarbonyl Lactones And Lactams Catalyzed By Chiral Pd(Ii)-Bisphosphine Complexes. J Org Chem. 2007 Jan 5;72(1):246-50.
合成参考文献
摘要:Chen, P.; Liu, G.; Engle, K. M.; Yu, J.-Q., Science of Synthesis Knowledge Updates, (2013) 2, 83. 摘要:Chen, P.; Liu, G.; Engle, K. M.; Yu, J.-Q., Science of Synthesis Knowledge Updates, (2013) 2, 94. 摘要:Chen, P.; Liu, G.; Engle, K. M.; Yu, J.-Q., Science of Synthesis Knowledge Updates, (2013) 2, 67. 摘要:Chen, P.; Liu, G.; Engle, K. M.; Yu, J.-Q., Science of Synthesis Knowledge Updates, (2013) 2, 77. 摘要:Chen, P.; Liu, G.; Engle, K. M.; Yu, J.-Q., Science of Synthesis Knowledge Updates, (2013) 2, 85.