Expedient synthesis of gem-dialkylbenzyl heterocycles through olefinic hydroarylation
作者:Yajing Lian、Kristen Burford、Allyn T. Londregan
DOI:10.1016/j.tet.2015.10.006
日期:2015.12
approach to gem-dialkylbenzyl heterocycles has been developed through a triflic acid-catalyzed hydroarylation of olefinic heterocycles. A broad range of substrates containing pyridine, quinoline, pyrazole, triazole and imidazole moieties are shown to be highly compatible with this method. This rapid construction of gem-dialkyl groups should be useful in the synthesis of drug-like molecules containing
通过三氟甲磺酸催化的烯烃杂环的加氢芳基化反应,已经开发出了一种健壮的方法,可用于制备宝石-二烷基苄基杂环。含有吡啶,喹啉,吡唑,三唑和咪唑部分的多种底物显示出与该方法高度相容。宝石-二烷基基团的这种快速构建在合成含有杂环多样性的类药物分子和研究宝石-二烷基效应中应该是有用的。