We reported an efficient synthesis of 2-functionalized benzoxazoles in mild condition and excellent yields. The synthetic process includes two steps. The step one contains a reaction of pendent halide formamidine derivatives and 2- aryloxyacetyl chloride generating highly selective (Z)-N-(2-halophenyl)-3-(dime- thyllamino)-2-aryloxyacrylamides, and the step two undergoes copper iodide catalyzed intramolecular C-O bond formation to yield title compounds. This strategy is not only providing newly discovered key intermediates 6a-l which contain multiple functional groups on 2-position (as building blocks), but also expanded the scope of methodologies for making diverse benzoxazoles with multiple functional groups.

中文翻译：

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碘化铜催化高效合成2-官能化苯并恶唑

我们报道了在温和条件下以优异的产率合成2-官能化苯并恶唑的方法。合成过程包括两个步骤。步骤1包含侧基卤甲酰胺衍生物与2-芳氧基乙酰氯的反应，生成高选择性（Z ）-N- （2-卤苯基）-3-（二甲基胸腺嘧啶）-2-芳氧基丙烯酰胺，并且步骤二进行碘化铜催化分子内CO键形成，得到标题化合物。该策略不仅提供了新发现的关键中间体6a-1 ，其在2-位上包含多个官能团（作为结构单元），而且扩展了制备具有多个官能团的各种苯并恶唑的方法范围。