Citation: He Shuwang, Yan Shiqiang, Guo Wei, Zhai Guangxi, Zhang Wei. One-Pot Synthesis of Amino Alcohols from Styrenes[J]. Chinese Journal of Organic Chemistry, ;2020, 40(7): 2094-2098. doi: 10.6023/cjoc202002028 shu

One-Pot Synthesis of Amino Alcohols from Styrenes

He Shuwang ^a ,
Yan Shiqiang ^b ,
Guo Wei ^c ,
Zhai Guangxi ^a,, ,
Zhang Wei ^b,,

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

Corresponding author: Zhai Guangxi, professorgxzhai@126.com Zhang Wei, zhangw416@fudan.edu.cn
Received Date: 22 February 2020
Revised Date: 6 May 2020
Available Online: 27 May 2020
Fund Project: 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)the National Major Scientific and Technological Special Project for "Significant New Drugs Development" No. 2018ZX09721003-008-026the National Key Research and Development Program of China No. 2018YFC0310900

Figures(2)

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%.
- amino alcohol,
- one-pot synthesis,
- 1, 3-dibromo-5, 5-dimethylhydantoin,
- styrene
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