作为手性中间体用于医药合成,具体应用于相关药物分子的构建。
医药
路线1:以1-(8-(苄氧基)-2-羟基喹啉-5-基)-2-溴乙酮为原料合成
- 步骤: 在氮气保护下,将四氢呋喃(1400 mL)和1-(8-(苄氧基)-2-羟基喹啉-5-基)-2-溴乙酮(100 g)的混合物冷却至0-5°C;缓慢加入R-甲基CBS(7.5 g),并在0-10°C下加入硼二甲基硫醚络合物(24.3 g);反应混合物在0-10°C下搅拌1-2小时,通过HPLC监测反应进程;反应完成后,缓慢加入甲醇(100 mL),并在0-10°C下继续搅拌15分钟;随后,在40-45°C的真空条件下蒸馏反应混合物,冷却至25-30°C;将冷却后的反应混合物缓慢加入盐酸溶液中,在25-30°C下搅拌1-2小时;过滤所得固体,用水(300 mL)洗涤,并在65-70°C下干燥8小时。
- 收率: 95%。
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