苯乙烯一锅法合成氨基醇  

One-Pot Synthesis of Amino Alcohols from Styrenes

作　　者：何淑旺 颜世强[2,3] 郭伟 翟光喜 张伟[2] He Shuwang;Yan Shiqiang;Guo Wei;Zhai Guangxi;Zhang Wei(College of Pharmacy,Shandong University,Jinan 250012;School of Pharmacy,Fudan University,Shanghai 201203;Shandong Dyne Marine Biopharmaceutical Co.,Ltd.,Weihai,Shandong 264300)

机构地区：[1]山东大学药学院,济南250012 [2]复旦大学药学院,上海201203 [3]山东达因海洋生物制药股份有限公司,山东威海264300

出　　处：《有机化学》2020年第7期2094-2098,共5页Chinese Journal of Organic Chemistry

基　　金：国家重点研究与发展计划(No.2018YFC0310900);国家科技重大专项“重大新药创制”(No.2018ZX09721003-008-026)资助项目.

摘　　要：报道了一种在丙酮和水的混合溶液中1,3-二溴-5,5-二甲基海因(DBH)催化烯烃两步一锅法合成氨基醇衍生物的新方法.室温条件下,苯乙烯衍生物首先与DBH反应0.5~2.0 h,然后与胺反应,最终能以64%~88%的收率得到相应的氨基醇.采用该方法以77%的收率完成了β2受体激动剂妥洛特罗克级的一锅法制备.A two-step one-pot procedure for the synthesis of amino alcohols mediated by 1,3-dibromo-5,5-dimethylhydantoin(DBH)in aqueous acetone solution was developed.Styrene derivatives were treated with DBH at room temperature for 0.5~2.0 h followed by the addition of amine,affording the corresponding amino alcohols in 64%~88%yields.Tulobuterol,a widely usedβ2-adrenergic agonist,was prepared by this protocol in gram scale with the yield of 77%.

关 键 词：氨基醇 一锅法合成 1 3-二溴-5 5-二甲基海因 苯乙烯 

分 类 号：O623.734[理学—有机化学]