📜1,2,3,4,6-戊-O-乙酰-A-D-吡喃半乳糖置于三甲基溴硅烷体系中,用 二氯甲烷 用作溶剂,化学反应 72.0H,以93%的收率获得2,3,4,6-四-O-乙酰基-1-溴-Alpha-D-甘露糖 参考文献:Rapid Preparation Of Variously Protected Glycals Using Titanium(III) 标题:Rapid Preparation Of Variously Protected Glycals Using Titanium(III) 摘要:Glycosyl Chlorides And Bromides Can Be Rapidly Converted To Glycals In High Yield By Reaction With (Cp2Ti[iii]Cl)(2). This Reagent Tolerates A Wide Range Of Common Carbohydrate Protecting Groups,Including Silyl Ethers,Acetals,And Esters; The Methodology Provides A General Route For The Preparation Of Glycals Substituted With Both Acid-And Base-Labile Functionality. A Reaction Mechanism Is Proposed That Is Based On Heteroatom Abstraction To Give An Intermediate Glycosyl Radical. This Radical Reacts With A Second Equivalent Of Ti(III) To Yield A Glycosyltitanium(Iv) Species. P-Heteroatom Elimination From The Glycosyltitanium(Iv) Complex Gives The Glycal. Doi:10.1021/jo982447K
专利号:US-5218097-A 优先权日:1988-12-07 标题:Process for the preparation of protected mono-sugar and oligo-sugar halides 发明人:ERNST BEAT 权利人:CIBA GEIGY CORP 摘要:The reaction of protected monosaccharides or oligosaccharides or protected monosaccharide and oligosaccharide derivatives containing an anomeric hydroxyl group with secondary α-haloenamines affords high yields of protected glycosyl halides, which are valuable intermediates for the introduction of sugar groups in the synthesis of oligosaccharides, glycolipids or glycopeptides.
专利号:US-6409990-B1 优先权日:1999-05-14 标 题:Macromolecular carrier for drug and diagnostic agent delivery 发明人:VERA DAVID R 权利人:UNIV CALIFORNIA 摘要:New macromolecular carriers for drugs and diagnostic agents are described that make use of the chemical attachment of new leashes to oligomeric backbone structures. The synthesis of these leashes and their facile creation, reaction and conjugation with chelators and ligands makes them ideal candidates for use in medicine, and especially diagnostics.
专利号:WO-03055887-A1 优先权日:2001-12-21 标 题:Conjugated porphyrin, chlorin or bacteriochlorin chromophore 发明人:BOYLE ROSS WILLIAM; GREENMAN JOHN 权利人:CATALYST BIOMEDICA LTD; BOYLE ROSS WILLIAM; GREENMAN JOHN 摘要:The invention provides a porphyrin, chlorin or bacteriochlorin chromophore, which chromophore comprises one conjugating meso substituent which comprises a conjugating group Z for covalently conjugating said chromophore to a protein so as to enable delivery of the chromophore to a selected biological target in vitro or in vivo, and one, two or three hydrophilic meso substituents, wherein the hydrophilicity of the chromophore is such that either on carrying out conjugation of said chromophore to said protein by way of incubating said chromophore and said protein for one hour under standard protein conjugation conditions in 10% DMSO/water buffered to pH 9, the percentage of non-covalently bound chromophore out of total protein-bound chromophore is 5% or less; or, where said protein is bovine serum albumin, on carrying out conjugation of said chromophore to said protein by way of incubating said chromophore and said protein for one hour under standard protein conjugation conditions in 10% DMSO/water buffered to pH 9, the percentage of non-covalently bound chromophore out of total protein-bound chromophore is 20% or less. The invention further provides methods for the synthesis of such chromophores, and methods for the use of such chromophores in therapy and in analysis.
专利号:US-4169197-A 优先权日:1977-09-06 标 题:6-Deoxyneamines aminoglycoside compounds 发明人:MAGERLEIN BARNEY J 权利人:UPJOHN CO 摘要:6-Deoxyneamine, 6-deoxy-5-epineamine, their 5-O-glycosyl derivatives, 6-deoxy-5-oxoneamine and the derivatives therefrom are useful as antibacterial agents and/or as intermediates in the synthesis of antibacterially active 6-deoxyneamines.
专利号:US-4232148-A 优先权日:1979-03-05 标题 :6-Deoxyneamines 发明人:MAGERLEIN BARNEY J 权利人:UPJOHN CO 摘要:6-Deoxyneamine, 6-deoxy-5-epineamine, their 5-0-glycosyl derivatives, 6-deoxy-5-oxoneamine and the derivatives therefrom are useful as antibacterial agents and/or as intermediates in the synthesis of antibacterially active 6-deoxyneamines.
专利号:US-4252970-A 优先权日:1977-09-06 标题:6-Deoxyneamines 发明人:MAGERLEIN BARNEY J 权利人:UPJOHN CO 摘要:6-Deoxyneamine, 6-deoxy-5-epineamine, their 5-0-glycosyl derivatives, 6-deoxy-5-oxoneamine and the derivatives therefrom are useful as antibacterial agents and/or as intermediates in the synthesis of antibacterially active 6-deoxyneamines.
参考标题:Large‐scale Synthesis Of Per‐O‐acetylated Saccharides And Their Sequential Transformation To Glycosyl Bromides And Thioglycosides 作者:Li‐cheng Huang,Pi‐hui Liang,Ching‐yang Liu,Chun‐cheng Lin |发布日期:2006.6 摘要:This Work Describes A Large‐scale Synthesis Of Per‐o‐acetylated Mono‐ And Disaccharides Using A Stoichiometric Amount Of Acetic Anhydride In The Presence Of Liclo4 Under Solvent‐free Conditions. The Peracetylated Saccharides Underwent Subsequent Anomeric Bromination And Thioglycosidation In One‐pot To Yield Synthetically Valuable Building Blocks.
合成参考文献
摘要:Schneider, C., Science of Synthesis, (2006) 24, 296. 摘要:Kryczka, B.; Lewkowski, J.; Zawisza, A., Science of Synthesis, (2007) 29, 992. 摘要:Gunn, S. J.; Warriner, S. L.; White, J. W., Science of Synthesis, (2007) 29, 912. 摘要:Kryczka, B.; Lewkowski, J.; Zawisza, A., Science of Synthesis, (2007) 29, 1034. 摘要:Merino, P., Science of Synthesis, (2007) 29, 714.