专利号:US-8097720-B2 优先权日:2008-12-24 标题:Process for the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid 发明人:PEGLION JEAN-LOUIS; DESSINGES AIMEE; SERKIZ BERNARD; LERESTIF JEAN-MICHEL; LECOUVE JEAN-PIERRE 权利人:PEGLION JEAN-LOUIS; DESSINGES AIMEE; SERKIZ BERNARD; LERESTIF JEAN-MICHEL; LECOUVE JEAN-PIERRE; LAB SERVER 摘要:Process for the synthesis of ivabradine of formula (I): n nand addition salts thereof with a pharmaceutically acceptable acid.
专利号:US-9567307-B2 优先权日:2011-01-07 标题:Amination of aryl alcohol derivatives 发明人:GARG NEIL K; RAMGREN STEPHEN D; SILBERSTEIN AMANDA L; QUASDORF KYLE W 权利人:GARG NEIL K; RAMGREN STEPHEN D; SILBERSTEIN AMANDA L; QUASDORF KYLE W; UNIV CALIFORNIA 摘要:Embodiments of the invention provide methods and materials for chemical cross-coupling reactions that utilize aryl alcohol derivatives as cross-coupling partners. Embodiments of the invention include methods for the amination of aryl sulfamates and carbamates, which are attractive cross-coupling partners, particularly for use in multistep synthesis. Illustrative embodiments include versatile means to use simple derivatives of phenol as precursors to polysubstituted aryl amines, as exemplified by a concise synthesis of the antibacterial drug linezolid.
专利号:US-2024368075-A1 优先权日:2021-07-02 标题 :Synthesis of N,N-Dialkyl, -Dialkenyl, -Dialkynyl, and Related Cyclics, Sulfamoyl Fluoride Compounds Using Hydrogen Fluoride 发明人:SINGH RAJENDRA P; HU QICHAO 权利人:SES HOLDINGS PTE LTD 摘要:Methods of producing N,N-dimethyl sulfamoyl fluoride and related derivatives of the formula F—S(O)2—NR2 (I) by contacting a sulfamoyl nonfluorohalide compound of the formula X—S(O)2—NR2 (II) with anhydrous hydrogen fluoride under conditions sufficient to produce the N,N-dimethyl sulfamoyl fluoride or derivative thereof of Formula I, wherein R in each of Formulas I and II is, independently, a linear or branched alkyl, alkenyl, or alkynyl group containing 1 to 12 carbon atoms, the Rs can be joined to form a cyclic amine with the N, and X is any one of chlorine, bromine, and iodine.
专利号:US-2023322661-A1 优先权日:2020-08-21 标题 :Synthesis of N,N-Branched Sulfamoyl Fluoride Compounds Using Bismuth Trifluoride 发明人:SINGH RAJENDRA P; HU QICHAO; SHEIMAN JOHNATHAN 权利人:SES HOLDINGS PTE LTD 摘要:Methods of producing N,N-branched sulfamoyl fluoride compounds of the formula F-S(O) 2 -NR 2 by contacting bismuth trifluoride with an N,N-branched sulfamoyl nonfluorohalide compound of the formula X-SO 2 NR 2 , wherein X=chlorine (Cl), bromine (Br), or iodine (I), and each R is, independently, a linear or branched alkyl, fluoroalkyl, alkenyl, fluoroalkenyl, alkynyl, or fluoroalkynyl with 1 to 12 carbon atoms, to fluorinate the N,N-branched sulfamoyl nonfluorohalide compound. This is a non-aqueous method, the purity of product is very high, and the desired product can be isolated in quantitative yield. The N,N-branched sulfamoyl fluoride compounds so produced are useful in various applications including as electrolyte solvents and additives in electrochemical devices, such as lithium batteries and capacitors, and in biological fields, among others.
专利号:US-6395918-B1 优先权日:1998-04-27 标题 :Conversion of a hydroxy group in certain alcohols into a fluorosulfonate ester or a trifluoromethylsulfonate ester 发明人:LOEWENTHAL HANS JACOB EDGAR; LOEWENTHAL RON BENJAMIN 摘要:The present invention provides a method of converting a hydroxy group in alcohols containing an electron withdrawing group into perfluoroalkane sulfonate and fluorosulfonate esters, which are good leaving groups, with inversion of configuration where the hydroxyl-bearing carbon is chiral. The method consists of converting an alcohol to an O—N,N-dialkylsulfamate ester and reacting it with a perfluoroalkansulfonic or fluorosulfonic acid. The method has applications in the synthesis of pharmaceutical and agrochemical compounds.
专利号:US-5359051-A 优先权日:1990-01-11 标题 :Compounds useful in the synthesis of nucleic acids capable of cleaning RNA 发明人:COOK PHILLIP D; GUINOSSO CHARLES J; BRUICE THOMAS 权利人:ISIS PHARMACEUTICALS INC 摘要:Compositions and methods for modulating the activity of RNA are disclosed. In accordance with preferred embodiments, antisense compositions are prepared comprising targeting and reactive portions. In preferred embodiments, the reactive portions comprise one or two imidazole functionalities conjugated to the targeting oligonucleotide via linkers with and without intervening intercalating moieties and act through phosphorodiester hydrolytic bond cleavage. Therapeutics, diagnostics and research methods are also disclosed. Synthetic nucleosides and nucleoside fragments are also provided which are useful for elaboration of oligonucleotides for such purposes.
摘要:Sainsbury, M., Science of Synthesis Knowledge Updates, (2010) 1, 255. 摘要:Mourad, A. K.; Czekelius, C., Science of Synthesis Knowledge Updates, (2011) 3, 78. 摘要:Guram, A. S.; Milne, J. E.; Tedrow, J. S.; Walker, S. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 81. 摘要:National Defense Research Committee, Office of Scientific Research and Development, Progress Report., NDCrc-132(Nov), 1942