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盐酸司来吉兰的合成 被引量:3

Synthesis of Selegiline Hydrochloride
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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%.
机构地区 中山大学药学院
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)
关键词 司来吉兰 合成 FRIEDEL-CRAFTS酰基化反应 手性源化合物 选择性B型单胺氧化酶抑制剂 selegiline synthesis Friedel-Crafts acylation chiral pool compound selective B monoamine oxidaseinhibitor
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参考文献10

  • 1Hajicek J, Hrbata J, Pihera P, et al. Method for the production of selegiline hydrochloride: EP, 0344675 [P]. 1991-01-09.
  • 2M·西蒂.药物制造百科全书[M].苏焕臣,曲秉杰,李晓东,等译.长春:长春出版社,1991:788.
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二级参考文献5

  • 1(美)M·西蒂著 苏焕臣 曲秉杰 李晓东译.药物制造百科全书[M].长春:长春出版社,1991.788.
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