摘要/Abstract

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.
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
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 used β2-adrenergic agonist, was prepared by this protocol in gram scale with the yield of 77%.
Key words: amino alcohol, one-pot synthesis, 1,3-dibromo-5,5-dimethylhydantoin, styrene


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