化学合成。
化学合成
合成路线 1（1. 合成：16096-33-6）
产率：99%
合成条件：With copper(II) acetate monohydrate; caesium carbonate In N,N-dimethyl-formamide at 110℃; for 24 h; Inert atmosphere
实验步骤：通用方法：在氮气下，向Cu（OAc）2 * H 2 O（0.01mmol）的DMF（2mL）溶液中加入芳基碘（1.2mmol），含氮杂环（1.0mmol）和Cs 2 CO 3（2mmol）。 大气层。 将混合物在110℃下搅拌24小时。 冷却至环境温度后，将混合物在水和乙酸乙酯之间分配。 分离有机层，水层用乙酸乙酯萃取。 将合并的有机层用盐水洗涤，用Na 2 SO 4干燥，并真空浓缩。 通过硅胶快速色谱法纯化残余物。
参考文献：
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合成路线 2（2. 合成：16096-33-6）
产率：91%
合成条件：With potassium carbonate In N,N-dimethyl-formamide at 120℃; for 12 h; Inert atmosphere
实验步骤：一般步骤：将芳基卤化物（1.0mmol），胺（1.5-2.0mmol），PNP-SSS（0.6mol％; 0.023g），K2CO3（2mmol）和DMF（3.0mL）置于装有磁性的25mL烧瓶中 搅拌棒并在氮气下在120℃下加热。 然后通过TLC监测反应直至检测到芳基卤的消耗。 反应完成后，向反应混合物中加入5mL水和5mL乙酸乙酯。 萃取有机溶液并经无水Na 2 SO 4干燥。 除去有机溶剂后，得到粗产物。 为了进一步纯化，使用色谱技术。
参考文献：
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合成路线 3（3. 合成：16096-33-6）
产率：96%
合成条件：With copper(II) oxide; potassium carbonate In N,N-dimethyl-formamide at 40℃; for 1.50 h;
实验步骤：一般步骤：在典型的N-芳基化方法中，将CuO NP（0.005g）加入到芳基卤（1.0mmol），吲哚/苯胺（1.0mmol）和K 2 CO 3（1.0mmol）在DMF（5mL）中的混合物中。 并在40℃下搅拌所需时间（表2）。 反应完成后，将反应混合物冷却至室温并用10mL水稀释并用乙酸乙酯（2×10mL）萃取。 将合并的有机萃取液用盐水洗涤，用无水MgSO 4干燥。 减压蒸发溶剂，通过柱色谱法纯化产物，得到所需纯度。 所有产物都是已知化合物，光谱数据与文献报道的相同.23-25将水层离心分离并回收催化剂用于下一次催化操作。
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