- 3'-硝基-4'-苄氧基-2-溴苯乙酮是福莫特罗的关键中间体,福莫特罗是一种长效的选择性肾上腺素β2受体激动药,具有支气管扩张作用,且呈剂量依赖关系,能使第1秒用力呼气量(FEV1)、用力肺活量(FVC)和呼气峰流速(PER)增加。
- 制备
步骤一:
在反应瓶中依次加入1000ml乙腈、150g 3-硝基-4-羟基苯乙酮和100g碳 酸钾,然后滴加100g溴化苄,升温700C搅拌反应;反应结束后,浓缩反应液,将反应液加入水 中,过滤、水洗、烘干,得到210g中间体1,收率为93%;
步骤二:
将200g中间体1加入到1000ml二氯甲烷中,加入277g三甲基苯基三溴化 铵,升温300C,反应4个小时;浓缩,将残留液加入到水中,过滤、水洗、烘干,得到253g 3'-硝基-4'-苄氧基-2-溴苯乙酮,收率为98%。
医药
合成路线 1(1. 合成:43229-01-2)
产率:98%
合成条件:With N,N,N-trimethylanilinium bromide In dichloromethane at 300℃; for 4 h;
实验步骤:步骤2:将200g中间体1加入到1000ml二氯甲烷中,加入277g三甲基苯基三溴化铵,温度升至300℃,反应进行4小时;将残余液体加入水中 过滤,水洗,干燥,得到253g 3-硝酸酯.Base 4-苄氧基-2-溴苯乙酮,收率98%;
参考文献:
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