摘要
3-甲氧基苯乙酮经还原胺化、(S)-扁桃酸拆分、Eschweiler-Clark反应及48%氢溴酸脱甲基,得到(S)-3-[(1-二甲胺基)乙基]苯酚,再与N-乙基-N-甲基氨甲酰氯经酰化后,与L-酒石酸成盐制得重酒石酸利斯的明,总收率约20%。
Rivastigmine hydrogen tartrate was synthesized from 3-methoxyacetophenone by reductive amination, resolution by （S）-mandelic acid, Eschweiler-Clark reductive methylation and then O-demethylation with 48%o hydrobromic acid to afford （S）-3-[- （1-dimethylamino）ethyl]phenol, which was subjected to acylation with N-ethyl-N-methylcarbamoyl chloride followed by L-tartaric acid salt formation with an overall yield of about 20 %.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2007年第5期327-329,共3页
Chinese Journal of Pharmaceuticals
关键词
重酒石酸利斯的明
乙酰胆碱酯酶抑制剂
阿尔茨海默病
合成
rivastigmine hydrogen tartrate
acetylcholine esterase （AchE） inhibitor
Alzheimer＇s disease
synthesis
