📜以 Neat (No Solvent) 用作溶剂,以81%的收率获得(乙酰氨基)乙酸甲酯 参考文献:Chemoselectivity In Coupling Of Azides With Thioacids In Solution-Phase And Solvent-Free Conditions 标题:Chemoselectivity In Coupling Of Azides With Thioacids In Solution-Phase And Solvent-Free Conditions 摘要:Solvent-Free Rapid Coupling Of Monothiocarboxylic Acid With Azide Affords Carboxamide Chemoselectively. Triphenyl Phosphine Included As An Additive Influences The Chemoselectivity,Yielding Carboxamide And Thioamide. Similar Variation In The Chemoselectivity Is Observed In The Absence And Presence Of Triphenyl Phosphine In Solution-Phase Methodology. Rapidity And Ecofriendliness Of The Solvent-Free Approach To Yield The Products In Just 15 Min Is Noteworthy Compared To The Solution-Phase Protocol,Which Has A Long Reaction Time (1-3 Days). Doi:10.1080/00397911.2011.606043
专利号:US-7737287-B2 优先权日:2002-03-28 标 题 :Anomeric derivatives of monosaccharides 发明人:MEUTERMANS WIM; WEST MICHAEL LEO; GIANG THANH LE; ADAMSON GEORGE; SCHAFER KARL; ABBENANTE GIOVANNI 权利人:ALCHEMIA LTD 摘要:This invention relates to combinatorial libraries of potentially biologically active mainly monosaccharide compounds and to methods of preparing same. These compounds are variously functionalized, with a view to varying lipid solubility, size, function and other properties, with the particular aim of discovering a drug or drug-like compound, or compounds with useful properties. The invention provides intermediates, processes and synthetic strategies for the solution or solid phase synthesis of monosaccharides, variously functionalized about the sugar ring, including the addition of aromaticity and charge, and the placement of amino acid and peptide side chain units of isosteres thereof.
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