顺序多组分组装过程/霍夫曼环加成策略在 1,2,3-三唑并[4,5-b] 苯并二氮杂䓬文库制备中的应用。
Application of a sequential multicomponent assembly process/huisgen cycloaddition strategy to the preparation of libraries of 1,2,3-triazole-fused 1,4-benzodiazepines.
机构信息
Department of Chemistry and Biochemistry, The Texas Institute for Drug and Diagnostic Development, The University of Texas, Austin, 78712, United States.
出版信息
ACS Comb Sci. 2012 Feb 13;14(2):135-43. doi: 10.1021/co2002087. Epub 2012 Feb 1.
Abstract
A strategy featuring a multicomponent assembly process followed by an intramolecular azide-alkyne dipolar (Huisgen) cycloaddition was implemented for the facile synthesis of three different 1,2,3-triazolo-1,4-benzodiazepine scaffolds. A diverse library of 170 compounds derived from these scaffolds was then created through N-functionalizations, palladium-catalyzed cross-coupling reactions, and several applications of α-aminonitrile chemistry.
摘要
采用多组分组装反应，然后进行分子内叠氮-炔二极（Huisgen）环加成反应，实现了三种不同的 1,2,3-三唑并-1,4-苯并二氮杂䓬骨架的简便合成。通过 N-官能化、钯催化交叉偶联反应以及α-氨基腈化学的几种应用，从这些骨架中衍生出了 170 种不同的化合物库。
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