摘要
提供了一条较为简洁的盐酸多奈哌齐合成路线,即以5,6-二甲氧基-2-(4-哌啶基甲基)-2,3-二氢-1H-茚酮为起始原料,PtO2催化氢化将吡啶还原为哌啶衍生物,以刘卡特-瓦拉赫反应为关键反应将胺基苄基取代制得盐酸多奈哌齐。再经过成盐和精制,以四步反应,69%的总收率得到了高质量的药用盐酸多奈哌齐。
To provide a concise synthetic route of donepezil hydrochloride.Firstly,to choose 5,6-dimethoxy-2-（4-piperidinyl methylene）-2,3-dihydro-1H-inden-1-one as the starting material,to reduce pyridine to piperidine derivative,by PtO2 hydrogenization.Secondly to prepare donepezil hydrochloride,by the key Leuckart-Wallach reaction.Finally,by salification and refination,to obtain the high quality pharmaceutical grade donepezil hydrochloride by four step reaction with a overall yield of 69%.
出处
《河北化工》
2012年第9期12-13,16,共3页
Hebei Chemical Industry
基金
国家"十二五"重大新药创制项目(2012ZX09201101-003)
关键词
盐酸多奈哌齐
阿尔茨海默病
刘卡特-瓦拉赫反应
精制
donepezil hydrochloride
aldo-keto reductase inhibitor
Leuckart-Wallach reaction
refination
