Imirestat, AL01576, Hoe-843, AL-1576
咪瑞司他Chemical Name: 2,5-Difluorospiro(fluoren-9,4'-imidazolidine)-2',5'-dione
CAS No. 89391-50-4, 96351-85-8 (AL-1576)
项目整合开发状态: Phase III
项目研究机构: Alcon (Originator)
合成路线:The reaction of 2,7-diaminofluorene (I) with NaNO2 and tetrafluoroboric acid in THF-water gives the bisdiazonium tetrafluoroborate (II),which by decomposition in refluxing xylene yields 2,7-difluorofluorene (III).The oxidation of (III) with KMnO4 in pyridine affords 2,7-difluoro-9-fluorenone (IV),which is cyclized with KCN and ammonium carbonate in refluxing ethanol.
📌 参考资料/链接：
参考文献标题:Spiro-tricycloaromatic succinimide derivs.as inhibitors of aldose reductase
文献作者:York,B.M.Jr.(Alcon Laboratories,Inc.)
参考来源:EP 0137333; ES 8800572; ES 8800915; ES 8900214; US 4537892
📄 详细内容
合成路线:The reaction of 2,7-diaminofluorene (I) with NaNO2 and tetrafluoroboric acid in THF-water gives the bisdiazonium tetrafluoroborate (II),which by decomposition in refluxing xylene yields 2,7-difluorofluorene (III).The oxidation of (III) with KMnO4 in pyridine affords 2,7-difluoro-9-fluorenone (IV),which is cyclized with KCN and ammonium carbonate in refluxing ethanol.
参考文献标题:Method of inhibiting aldose reductase activity,compsns.therefor and process for preparing spiro-fluorofluoren and spiro-difluorofluoren cpds.
文献作者:York,B.M.Jr.(Alcon Laboratories,Inc.)
参考来源:WO 8303543
合成路线:The reaction of 2,7-diaminofluorene (I) with NaNO2 and tetrafluoroboric acid in THF-water gives the bisdiazonium tetrafluoroborate (II),which by decomposition in refluxing xylene yields 2,7-difluorofluorene (III).The oxidation of (III) with KMnO4 in pyridine affords 2,7-difluoro-9-fluorenone (IV),which is cyclized with KCN and ammonium carbonate in refluxing ethanol.
参考文献标题:IMIRESTAT < Prop INN >
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1989,14(3),226
产品链接: CAS No. 89391-50-4››