布格呋喃体内代谢产物的合成

发布时间：2018-05-06 22:34

本文选题：布格呋喃 + AF-　；参考：《中国药科大学学报》2016年06期

【摘要】：布格呋喃(AF-5)是已报道的一类具有抗焦虑活性的精神治疗药物之一,其结构由一个沉香呋喃环骨架和一个正丁基侧链组成。临床药代研究发现其新的代谢产物,推测其结构可能为烷烃链端基的羰酸化产物。为了确证其结构,以中间体(4a R,7R,8a R)-8a-羟基-7-(2-羟丙基-2-基)-4a-甲基八氢萘-2(1氢)-酮为原料,经6步反应,成功合成了目标化合物,总收率16.7%。化合物的结构均经NMR和MS确证。
[Abstract]:Bugfuran (AF-5) is one of the reported psychotherapeutic drugs with antianxiety activity. Its structure consists of a cytoskeleton and a positive side chain of Ding Ji. New metabolites were found in clinical pharmacokinetic studies, which suggested that their structures might be carbonylation products of alkane chain terminal groups. In order to confirm its structure, the target compound was successfully synthesized from the intermediate 4a Rn 7RN 8a RZ-8a- hydroxypropyl -2-hydroxypropyl -4a- methyloctachloronaphthalene -2H _ 2H _ 2N _ 1 through six steps reaction, with the overall yield of 16.7b. The structures of the compounds were confirmed by NMR and MS.
【作者单位】：中国医学科学院北京协和医学院药物研究所活性物质发现与适药化北京市重点实验室;北京积水潭医院;
【基金】：国家“重大新药创制”科技重大专项资助项目(No.2010ZX09401405-001)~~
【分类号】：R914.5

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