三氯化铁催化选择性合成普罗布考单丁二酸酯(英文)  

Iron trichloride-assisted selective synthesis of 4-(2,6-di-tertbutyl-4-(2-(3,5-di-tertbutyl-4-hydroxyphenylthio)propan-2-ylthio)phenoxy)-4-oxobutanoic acid

作　　者：孙秋[1] 罗新峰[1] 尹海滨 黄文才[3] 

机构地区：[1]四川大学华西药学院靶向药物及释药系统教育部重点实验室,四川成都610041 [2]广州市元通医药科技有限公司,广东广州510610 [3]四川大学化工学院,四川成都610065

出　　处：《化学研究与应用》2011年第5期559-563,共5页Chemical Research and Application

基　　金：广东省教育部产学研结合项目(2007B090400016)资助

摘　　要：研究了以三氯化铁为催化剂选择性合成普罗布考单丁二酸酯的反应。考察了催化剂、反应溶剂、碱、酰化剂及配料比对反应的影响。实验结果表明金属盐对反应的收率和单酰化反应的选择性有显著的影响,当以三氯化铁为催化剂,丁二酸酐为酰化剂,叔丁醇钠为碱,四氢呋喃为溶剂,普罗布考、叔丁醇钠、丁二酸酐及三氯化铁的摩尔比为1∶4∶5∶0.17,反应温度为室温,反应时间为1h时,普罗布考单丁二酸酯的产率可达55%。The selective mono-acylation of probucol by succinic anhydride was studied.Effects of metal salt,solvent,base and acylating agent had been investigated.It was found that the metal salt affected the yield and selectivity of acylation markedly.The reaction conditions were also optimized.When the mole ratio of probucol,sodium tert-butoxide,succinic anhydride and iron trichloride was 1∶4∶5∶0.17,and the acylation was carried out in THF for 1 hour at room temperature,the yield of probucol monosuccinate was 55%.

关 键 词：普罗布考 普罗布考单丁二酸酯 单酰化 三氯化铁 区域选择性 

分 类 号：O621.31[理学—有机化学]