4-己基间苯二酚的合成工艺改进  

Improved Synthetic Process of 4-Hexylresorcinol

作　　者：简杰[1] 杨晖[1] 许文东 杨兆琪[3] 孙平华[1] 

机构地区：[1]暨南大学药学院,广东广州510632 [2]广州白云山汉方药业,广东广州510000 [3]江南大学食品学院,江苏无锡214122

出　　处：《中国医药工业杂志》2016年第6期685-686,共2页Chinese Journal of Pharmaceuticals

基　　金：广州市产学研协同创新重大专项(201508020128);广东省教育厅重点平台及特色创新项目(2015KTSCX013);江苏省自然科学基金(BK20130121)

摘　　要：间苯二酚(2)和正己酸为原料,依次经酰化、还原反应制得驱虫药4-己基间苯二酚。酰化反应中将传统催化剂换成三氟化硼乙醚复合物,反应温度可由120℃降低到100℃,且常压即可反应,定量制得4-己酰间苯二酚。第二步还原反应中,以雷尼镍/氢气代替锌汞齐作还原剂,反应时间短,试剂价廉易得并可回收反复使用。改进后的工艺条件温和,原料易得,无需使用特殊的低温或加压装置,整个过程设备要求简单,产品易于分离,适合工业化生产,总收率86%。The anthelmintic 4-hexylresorcinol was prepared from resorcinol （2） and caproic acid via Friedel- Crafts acylation and reduction. The 4-hexanoylresorcinol （3） was quantitatively yielded at constant pressure with the reaction temperature lowered from 120 ℃ to 100 ℃ while the conventional catalysts was replaced by EtzO-BF3 in acylation. The reaction time was shorten in the second reduction reaction with the cheap and recyclable reagent Raney nickel/hydrogen instead of zinc amalgam as reducing agent. The improved process was performed at mild reaction conditions, simplified operational equipment and cheap raw materials without using special low temperature or pressure device, therefore it is very suitable for industrialized production with an overall yield about 86 % （based on compound 2）.

关 键 词：4-己基间苯二酚 驱虫药 合成 

分 类 号：R914[医药卫生—药物化学]