Silver Benzoate置于吡啶,Boron Fluoride Ether,苯体系中,化学反应生成 1-乙酰氧基-2,3,5-三苯甲酰氧基-1-Beta-D-呋喃核糖 参考文献:Ribofuranose Derivatives From 3,5-Di-O-Benzoyl-D-Ribosyl Chloride. I. 1,3,5-Tri-O-Benzoyl-β-D-Ribose And 5-O-Benzoyl-1,2,3-O-Benzylidyne-α-D-Ribose*1 标题:Ribofuranose Derivatives From 3,5-Di-O-Benzoyl-D-Ribosyl Chloride. I. 1,3,5-Tri-O-Benzoyl-β-D-Ribose And 5-O-Benzoyl-1,2,3-O-Benzylidyne-α-D-Ribose*1 摘要: DOI:10.1021/jo01362A039
专利号:EP-1709057-B1 优先权日:2004-01-21 标 题:Synthesis of spongosine 发明人:OUZMAN JACQUELINE VALERIE ANNE 权利人:CAMBRIDGE BIOTECHNOLOGY LTD 摘要:Reaction of 1-O-acetyl-2,3,5-tri-O-benzoyl-β-D-ribofuranose with 2-methoxyadenine to form 9-(2′,3′,5′-tri-O-benzoyl-β-D-ribofuranosyl)-2-methoxyadenine, then deprotection of the 9-(2′,3′,5′-tri-O-benzoyl-β-D-ribofuranosyl)-2-methoxyadenine to form spongosine is described. Synthesis of intermediates for use in the synthesis of spongosine is also described.
专利号:US-9266863-B2 优先权日:2010-03-30 标题 :Process for the synthesis of azacitidine and decitabine 发明人:DE FERRA LORENZO; ZENONI MAURIZIO; TURCHETTA STEFANO; ANIBALDI MAURO; AMMIRATI ETTORE; BRANDI PAOLO; BERARDI GIORGIO 权利人:DE FERRA LORENZO; ZENONI MAURIZIO; TURCHETTA STEFANO; ANIBALDI MAURO; AMMIRATI ETTORE; BRANDI PAOLO; BERARDI GIORGIO; CHEMI SPA 摘要:Described herein is a process for the synthesis of azacitidine or decitabine, comprising the silylation of azacytosine in the presence of N,O-bis-trimethylsilyl-trifluoroacetamide. Such reaction is performed in an organic solvent, preferably aprotic, even more preferably selected from among dichloromethane, dichloroethane and/or acetonitrile. According to a further aspect of the process, 2 to 3 moles of N,O-bis-trimethylsilyl-trifluoroacetamide are used per mole of azacytosine, preferably from 2.2 to 2.5.
专利号:EP-0948511-B1 优先权日:1996-12-24 标 题:Chemical synthesis of nucleosides analogs and their incorporation into polynucleotides 发明人:KARPEISKY ALEXANDER; BEIGELMAN LEONID; MATULIC-ADAMIC JASENKA 权利人:SIRNA THERAPEUTICS INC 摘要:Novel nucleosides, process for chemical synthesis of nucleosides and incorporation of the nucleosides into polynucleotides are disclosed. Also described are polynucleotides, such as antisense, TFO and nucleic acid catalysts with one or more modifications, such as 2'-O-amino, L-nucleotides and the others.
专利号:US-7855285-B2 优先权日:2005-06-14 标 题:Methods for selective N-9 glycosylation of purines 发明人:ROBINS MORRIS J; ZHONG MINGHONG 权利人:UNIV BRIGHAM YOUNG 摘要:A process for providing regiospecific and highly stereoselective synthesis of 9-β anomeric purine nucleoside analogs is described. The introduction of the sugar moiety on to 6-(azolyl)-substituted purine bases is performed so that highly stereoselective formation of the β anomers of only the 9 position regioisomers of the purine nucleoside analogs (either D or L enantiomers) is obtained. This regiospecific and stereoselective introduction of the sugar moiety allows the synthesis of nucleoside analogs, and in particular 2′-deoxy, 3′-deoxy, 2′-deoxy-2′-halo-arabino and 2′,3′-dideoxy-2′-halo-threo purine nucleoside analogs, in high yields without formation of the 7-positional regioisomers. Processes for providing novel 6-(azolyl)purines for the regiospecific and highly stereoselective synthesis of 9-β anomeric purine nucleoside analogs are described. The compounds are drugs or intermediates to drugs.
专利号:US-6177409-B1 优先权日:1996-07-05 标 题 :Method for the site specific synthesis of novel 3-hydroxypyridin-4(1H)ons derivatives from aminomonosaccharides or aminoitols, products obtained by this method and their applications 发明人:VANLEMMENS PIERRE PAUL; POSTEL DENIS GHISLAIN; GERMAIN PIERIG EMMANUEL; JULIEN RENE JEAN-MARIE; PETIT JEAN-PIERRE CONSTANT; RONCO GINO LINO; VILLA PIERRE JOSEPH 权利人:INST BIOCHIMICO PAVESE PHARMA 摘要:Process for regiospecific preparation of new 3-hydroxypyridine-4(1H)-one derivatives starting from monosaccharides or itols of general formula:in which R represents a radical, either saturated or not, branched or not, having carbon-atom groups, and having hetero-atoms or not, and Sub represents a saccharide derivative or an itol, either cyclic not, protected or not, the hydrocarbon skeleton of which is bound to the nitrogen atom of the pyridinone either directly or by the intermediary of a spacing group. The present invention is characterized in that the process comprises a first step of protection of the 3-hydroxy group of the pyranone derivative, a second basocatalyzed step of substitution of the intracyclic oxygen atom of the pyranone by the nitrogen atom of the amine function of the amino monosaccharide or amino itol, and a third step of de-protection of the 3-OH group of the pyridinone cycle and possibly of the OH groups of the glucide or itol residue. It also regards the products obtained by this process, as well as their applications, namely as medicaments for the treatment of toxic overloads of FeIII.
专利号:US-9109000-B2 优先权日:2012-11-09 标题:Synthesis of nucleosides 发明人:POZZOLI CLAUDIO GIANLUCA; CANEVARI VALENTINA; BRUSASCA MARCO; MENNA LORENZO; CURTI MATTEO 权利人:FARMABIOS SPA; FARMABIOS SPA 摘要:A process for the preparation of nucleosides, derivatives and analogues thereof by coupling reaction of a protected suitable nitrogeneous purine or pyrimidine base, a derivative or analogue thereof and a protected suitable sugar in the presence of SnCl 4 comprising the removal of SnCl4 by adding DMSO directly into the reaction mixture is described. Preferably said process is used for the preparation of antiviral and antitumor agents having a nucleoside or nucleoside-like structure, still more preferably for the preparation of azacytidine, decitabine, chlorfarabine, cladribine, mizoribine. A residual tin content lower than 300 ppm is obtained with said process.