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溴化铜存在下,对异丁基苯丙酮(2)、乙二醇和过溴型三甲基苄铵树脂一锅反应转化成2-(1-溴乙基)-2-(4-异丁基苯基)-1,3-二氧戊环(3),再经重排、水解即得布洛芬(1),以异丁基苯丙酮计算,总收率88.7%。探讨了反应温度,溴化铜的用量对(3)收率的影响。还考察了添加不同Lewis酸对无水乙酸锌催化(3)重排时间的影响。
A one-pot reaction of isobutylpropiophenone (2), ethylene glycol, and perbromomethyltrimethylbenzyl ammonium chloride was converted to 2- (1-bromoethyl) -2- (4-isobutyl (3), and then by rearrangement, hydrolysis ibuprofen (1), with isobutylpropiophenone, the total yield of 88.7%. The effects of reaction temperature and amount of copper bromide on the yield of (3) were discussed. The effect of adding different Lewis acids on the catalytic (3) rearrangement time of anhydrous zinc acetate was also investigated.