8-溴甲基喹啉是合成8-喹啉甲胺二盐酸盐的中间体,是8-喹啉甲胺的盐形式。8-喹啉甲基胺用于制备喹唑啉酮衍生物作为抗肿瘤药物。
医药
合成路线 1(1. 合成:7496-46-0)
产率:46%
合成条件:With N-Bromosuccinimide; dibenzoyl peroxide In cyclohexane for 10 h; Inert atmosphere; Reflux
实验步骤:在N 2气氛下,向过度干燥的300mL三颈烧瓶中加入8-甲基喹诺酮(10.0g,69.8mmol),过氧化苯甲酰(0.843g,3.49mmol)和环己烷(150mL)。 然后在搅拌下分批加入N-溴代琥珀酰亚胺(13.6g,76.8mmol)。 将溶液回流10小时。 反应完成后,过滤反应混合物,滤液用饱和NaHCO 3水溶液(3×100mL)和盐水(100mL)洗涤,并经无水Na 2 SO 4干燥。 将溶剂真空蒸发。 用Et 2 O和己烷重结晶,得到浅棕色固体(7.1g,46%)。
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