PHYSOSTIGMINE AND ANALOGS

毒扁豆碱及其类似物

• 批准号: 3876465
• 负责人: A BROSSI
• 金额: --
• 依托单位: NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES
• 依托单位国家: 美国
• 资助国家: 美国
• 起止时间: 至
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/3876465
• 关键词: carbamates; cholinesterase inhibitors; drug design /synthesis /production; drug metabolism; oxazine; physostigmine

Novel carbamates of N(l)-norphysostigmine of the (-)-series were prepared. Both, the butyl- and the octyl-analog were found to be highly potent in vitro in inhibiting cholinesterases. Synthesis of (+)physovenine from intermediates of the physostigmine synthesis was accomplished. Synthesis of optically active material by phase-transfer induced chirality has been achieved. Synthesis of natural N(8)norphysostigmine from 5-methoxy-N-methyltryptamine has been initiated and led to (+)-N(8)-noreseroline methyl ether. Resolution by the phenylethylurea method is planned.

合成了(-)-系列的N(L)-去甲壳胺氨基甲酸酯类化合物。 丁基和辛基类似物都被发现在 体外抑制胆碱酯酶活性。(+)酸模精氨酸的合成 完成了毒扁豆碱的中间体合成。一种新的合成方法 通过相转移诱导手性的光学活性材料已经被 已实现。天然N(8)去甲肾上腺素的合成 5-甲氧基-N-甲基色胺已被启动并导致 (+)-N(8)-去甲氧胆碱甲醚。苯乙基脲拆分 方法是有计划的。