Flutropium bromide, Ba 598 Br, Flubron
氟托溴铵 Chemical Name: endo-8-(2-Fluoroethyl)-3-(2-hydroxy-2,2-diphenylacetoxy)-8-methyl-8-azoniabicyclo[3.2.1]octane bromide
CAS No. 63516-10-9 (anti-isomer), 63516-07-4 (syn-isomer)
项目整合开发状态: Launched-1988
项目研究机构: Boehringer Ingelheim (Originator), SSP (Licensee)
合成路线:The esterification of N-benzyloxycarbonylnortropine (II) with diphenyl chloroacetic acid (I) gives the corresponding ester (III),which is deprotected and hydrolyzed to afford nortropine benzylate (IV).This compound (IV) is alkylated with 2-bromo-1-fluoroethane (V) by means of Na2CO3 in refluxing acetonitrile yielding N-(2-fluoroethyl)nortropine benzylate (VI),which is finally treated with methyl bromide in dichloromethane acetonitrile.
📌 参考资料/链接：
参考文献标题:Quaternary N-beta-substd.benzylic acid N-alkyltropinic esters
文献作者:Banholzer,R.; Bauer,R.; Heusner,A.; Schulz,W.(Boehringer Ingelheim GmbH)
参考来源:DE 2540633
📄 详细内容
合成路线:The esterification of N-benzyloxycarbonylnortropine (II) with diphenyl chloroacetic acid (I) gives the corresponding ester (III),which is deprotected and hydrolyzed to afford nortropine benzylate (IV).This compound (IV) is alkylated with 2-bromo-1-fluoroethane (V) by means of Na2CO3 in refluxing acetonitrile yielding N-(2-fluoroethyl)nortropine benzylate (VI),which is finally treated with methyl bromide in dichloromethane acetonitrile.
参考文献标题:Flutropium Bromide
文献作者:Castar,J.; Serradell,M.N.; Castar,R.M.
参考来源:Drugs Fut 1987,12(7),630
合成路线:The esterification of N-benzyloxycarbonylnortropine (II) with diphenyl chloroacetic acid (I) gives the corresponding ester (III),which is deprotected and hydrolyzed to afford nortropine benzylate (IV).This compound (IV) is alkylated with 2-bromo-1-fluoroethane (V) by means of Na2CO3 in refluxing acetonitrile yielding N-(2-fluoroethyl)nortropine benzylate (VI),which is finally treated with methyl bromide in dichloromethane acetonitrile.
参考文献标题:Synthesis of the bronchospasmolytic agent flutropim bromide and of some homologous and configuration isomeric compounds
文献作者:Banholzer,R.; et al.
参考来源:Arzneim-Forsch Drug Res 1986,36(8),1161-6
产品链接: CAS No. 63516-10-9›› 产品链接: CAS No.63516-07-4››