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萘普生合成工艺改进
IMPROVED SYNTHESIS OF dl-NAPROXEN
【摘要】 为避免前文工艺中缩酮化和重排反应耗时长的缺点,将反应步骤改为丙酰萘甲醚先缩酮化后再溴化;所得溴代缩酮4再用氯化锌在甲苯中重排,从而使反应周期缩短30h 以上,总收率高,并割除了原甲酸三乙酯。
【Abstract】 The ketalization of 2-propionyl-6-methoxynaphthalene(2)affordedthe ethylene ketal(3),which was brominated to give the bromoketal(4).Therearrangement of 4 followed by saponification and acidification provided naproxenin high overall yield.This process has the advantage of shorter reaction periodand does not require the expensive ethyl orthoformate.
【关键词】 萘普生;
合成;
缩酮化;
溴化;
重排;
位阻;
【Key words】 napoxen; synthesis; ketalization; bromination; rearrangement; steric hindrance;
【Key words】 napoxen; synthesis; ketalization; bromination; rearrangement; steric hindrance;
- 【文献出处】 医药工业 , 编辑部邮箱 ,1988年11期
- 【被引频次】8
- 【下载频次】371