摘要
目的:设计一种以苯为原料合成单胺氧化酶(monoamine oxidase,MAO)抑制剂中间体1,2,3,4-四氢萘-1-胺盐酸盐的方法。方法:采用Fridel-Crafts酰化反应、Wolf-Kishner-黄明龙还原反应和Harwoth环合反应等方法,以苯为原料,经酰化、还原、环合、缩合、还原以及成盐制得1,2,3,4-四氢萘-1-胺盐酸盐(11)。结果:合成(11)的总收率为43.6%。结论:建立了合成MAO抑制剂中间体1,2,3,4-四氢萘-1-胺盐酸盐的方法,该方法具有原材料廉价易得、反应操作简便以及产品收率较高且品质好等优点,具有一定的工业化生产前景。
Objective:To design a method for synthesizing 1,2,3,4-tetrahydro-l-naphthalenamine hydrochloride, which is an impor-tant intermediate for monoamine oxidase (MAO) inhibitors. Methods: 1,2,3,4-tetrahydro-1-naphthylamine hydrochloride ( 11 ) was synthesized from benzene via acylation, reduction,cyclization, condensation, reduction,and salification by methods of Fridel Crafts acylation,Wolf-kishner-HUANG Minglong reduction and Harwoth cyclization. Results:Overall yield for synthesizing 1,2,3,4-te-trahydro-1-naphthylamine hydrochloride ( 11 ) was 43.6%. Conclusions: Method for synthesizing 1,2,3,4-tetrahydro - 1 -naphthale-namine hydrochloride is establish. Optimized synthetic route has advantages in industrial production for its cheap and readily available raw materials, easy in operation, high yield and high quality of products.
出处
《重庆医科大学学报》
CAS
CSCD
北大核心
2013年第6期580-582,共3页
Journal of Chongqing Medical University
基金
国家科技重大专项课题"重大新药创制"资助项目(编号:2010ZX09401-306-1-1)
关键词
单胺氧化酶抑制剂
中间体
1
2
3
4-四氢萘-1-胺
合成
monoamine oxidase inhibitor
intermediate
1
2
3
4-tetrahydro-1-naphthylamine hydrochloride
synthesize