Chinese Journal of Organic Chemistry ›› 2020, Vol. 40 ›› Issue (7): 2094-2098.DOI: 10.6023/cjoc202002028 Previous Articles     Next Articles


何淑旺a, 颜世强b,c, 郭伟c, 翟光喜a, 张伟b   

  1. a 山东大学药学院 济南 250012;
    b 复旦大学药学院 上海 201203;
    c 山东达因海洋生物制药股份有限公司 山东威海 264300
  • 收稿日期:2020-02-22 修回日期:2020-05-06 发布日期:2020-05-29
  • 通讯作者: 翟光喜, 张伟;
  • 基金资助:

One-Pot Synthesis of Amino Alcohols from Styrenes

He Shuwanga, Yan Shiqiangb,c, Guo Weic, Zhai Guangxia, Zhang Weib   

  1. a College of Pharmacy, Shandong University, Jinan 250012;
    b School of Pharmacy, Fudan University, Shanghai 201203;
    c Shandong Dyne Marine Biopharmaceutical Co., Ltd., Weihai, Shandong 264300
  • Received:2020-02-22 Revised:2020-05-06 Published:2020-05-29
  • Supported by:
    Project supported by the National Key Research and Development Program of China (No. 2018YFC0310900) and the National Major Scientific and Technological Special Project for "Significant New Drugs Development" (No. 2018ZX09721003-008-026).

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