首页 | 本学科首页   官方微博 | 高级检索  
检索        

1-(4-甲基苄基)-2-甲基-八氢异喹啉盐酸盐的合成
引用本文:刘为中,何广卫,王银虎,何建勋,王奎.1-(4-甲基苄基)-2-甲基-八氢异喹啉盐酸盐的合成[J].中国药科大学学报,2016,47(5):548-550.
作者姓名:刘为中  何广卫  王银虎  何建勋  王奎
作者单位:合肥医工医药有限公司,合肥医工医药有限公司,合肥医工医药有限公司,合肥医工医药有限公司,合肥医工医药有限公司
摘    要:化合物1-(4-甲基苄基)-2-甲基-八氢异喹啉盐酸盐(1)是制备新型镇咳药磷酸二甲啡烷的关键中间体。对化合物1的合成工艺进行研究,以4-甲基苯乙酸为原料,采用氯化亚砜氯代制得4-甲基苯乙酰氯,再与2-环己烯基乙胺反应,再经环化、还原、N-甲基化和成盐酸盐纯化得到目标产物1,总收率约54%,纯度大于98%。该工艺具有原料易得、操作简便、产率和纯度高、成本低等优点,适合工业化生产。

关 键 词:磷酸二甲啡烷  中间体  合成  镇咳药

Synthesis of 1-(4-methylbenzyl)-2-methyl-octahydro-isoquinoline hydrochloride
LIU Weizhong,HE Guangwei,WANG Yinhu,HE Jianxun and WANG Kui.Synthesis of 1-(4-methylbenzyl)-2-methyl-octahydro-isoquinoline hydrochloride[J].Journal of China Pharmaceutical University,2016,47(5):548-550.
Authors:LIU Weizhong  HE Guangwei  WANG Yinhu  HE Jianxun and WANG Kui
Abstract:1-(4-Methylbenzyl)-2-methyl-octahydro-isoquinoline hydrochloride(1)is the key intermediate to prepare a new type of antitussives agent phosphate dimemorfan. 4-methyl-phenylacetic acid as a raw materials, was chlorinated with thionyl chloride to obtain 4-methyl-phenylacetyl chloride, followed by reaction with 2-cyclohexenyl amine, then cyclization, reduction, methylation and salt formation by HCl were taken out to give the desired product 1. The total yield is 54%, and the purity is greater than 98%. This synthetic process is characterized with available raw materials, simple in operation with high yield and purity, and suitable for large-scale production.
Keywords:phosphate dimemorfan  intermediate  synthesis  antitussive agent
点击此处可从《中国药科大学学报》浏览原始摘要信息
点击此处可从《中国药科大学学报》下载免费的PDF全文
设为首页 | 免责声明 | 关于勤云 | 加入收藏

Copyright©北京勤云科技发展有限公司  京ICP备09084417号