作为医药中间体或活性成分,用于相关药物研发与生产。
医药
合成路线 1(1. 合成:1316216-05-3)
产率:38%
合成条件:With caesium carbonate In tetraethoxy orthosilicate at 140℃; for 14 h;
实验步骤:将化合物2(6.2g,25mmol),碘苯(6.12g,30mmol),Cul(955mg,5.0mmol),CS2CO3(16.3g,50mmol)在TEOS(200ml)中的混合物脱气并吹扫 用氮气。 将所得混合物在140℃下搅拌14小时。 冷却至室温后,将残余物用EtOAc(200ml)和95%EtOH(200ml),NH 4 F-H 2 O在硅胶上稀释[50g,通过在水(1500ml)中加入NH 4 F(100g)预制备至二氧化硅。 加入凝胶(500g,100-200mesh)],并将得到的混合物在室温下保持2小时,过滤固化的物质并用EtOAc洗涤。 将滤液蒸发至干,通过硅胶色谱法(石油醚/ EtOAc = 10/1)纯化残余物,得到黄色固体(3g,38%)。
参考文献:
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