广东药学院学报2012，Vol.28Issue(2)：135-137,3.DOI:10.3969/j.issn.1006-8783.2012.02.007
盐酸右美托咪定的合成
Synthesis of dexmedetomidine hydrochloride
摘要
Abstract
Objective To optimize the process of preparing medetomidine(l) for industrial production,which is an important intermediate of dexmedetomidine hydrochloride. Methods Improved Friedel-Crafts Reaction was employed to obtain compound 1 with N-( trimethylsilyl) imidazole (TMSI) as a raw material. Solvents and Lewis acid as catalyst were investigated for high yields. Results The optimal conversion ratio of Friedel-Crafts Reaction was achieved to be 66. 3% with BF3OEt2/CH2Cl2 as the catalyst. The product was confirmed to be the right structure via IR, NMR and elemental analysis. Conclusion The research shows that it is possible to get access to a relatively cheap reactant and a reasonable high conversion rate for the target product. Therefore it may be a sustainable method for the large scale industrial production.
关键词
盐酸右美托咪定/美托咪定/Friedel-Crafts反应/N-三甲基硅咪唑Key words
dexmedetomidine hydrochloride/ medetomidine/ Friedel-Crafts reaction/N-( trimethylsilyl)imidazole分类
药学引用本文复制引用
王玉平,冯颂延,林丽薇..盐酸右美托咪定的合成[J].广东药学院学报,2012,28(2):135-137,3.
