摘要
以N-Fmoc-D-丙氨酸为手性源,经过Friedel-Crafts酰基化、脱保护和还原反应得(R)-?-甲基苯乙胺,然后经炔丙基化及还原甲基化反应制得选择性B型单胺氧化酶抑制剂盐酸司来吉兰,总收率约41%。
Selegiline hydrochloride, a selective B monoamine oxidase inhibitor, was synthesized from the chiral pool compound N-Fmoc-D-alanine via Friedel-Crafts acylation, deprotection and reduction to give (R)-α- methylphenethylamine, which was subjected to propargylation and reductive methylation with an overall yield of 41%.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2015年第9期943-945,共3页
Chinese Journal of Pharmaceuticals
基金
国家自然科学基金资助项目(21172270
21202208和21472248)