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2013 , Vol. 33 >Issue 03: 634 - 639

DOI: https://doi.org/10.6023/cjoc201211015

研究简报

β2-AR激动剂BI-167107的合成

  • 王江波 ,
  • Seungkirl Ahn ,
  • Alem W.Kahsai ,
  • 刘蓉 ,
  • 任杰 ,
  • 胡昆 ,
  • 孙小强 ,
  • 陈新
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  • a 常州大学制药与生命科学学院 常州 213164;
    b Department of Medicine, Duke University Medical Center, Durham, NC 27710, USA;
    c 常州大学石油化工学院 常州 213164

收稿日期: 2012-11-18

  修回日期: 2012-12-06

  网络出版日期: 2012-12-20

基金资助

国家自然科学基金(Nos. 21272029, 81272982)资助项目.

收起

Synthesis of β2-AR Agonist BI-167107

  • Wang Jiangbo ,
  • Ahn Seungkirl ,
  • Kahsai Alem W. ,
  • Liu Rong ,
  • Ren Jie ,
  • Hu Kun ,
  • Sun Xiaoqiang ,
  • Chen Xin
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  • a School of Pharmaceutical and Life Science, Changzhou University, Changzhou 213164;
    b Department of Medicine, Duke University Medical Center, Durham, NC 27710, USA;
    c School of Petrochemical Engineering, Changzhou University, Changzhou 213164

Received date: 2012-11-18

  Revised date: 2012-12-06

  Online published: 2012-12-20

Supported by

Project supported by the National Natural Science Foundation of China (Nos. 21272029, 81272982).

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摘要

BI-167107是一种新的长效β2肾上腺素受体(β2-AR)激动剂, 在鉴定G蛋白偶联受体(GPCR)/配体络合物的结构方面具有重要应用. 以2-硝基间苯二酚为原料, 经过七步反应, 合成了目标化合物, 其结构经1H NMR, 13C NMR和MS确证. 此合成路线的优点是避免了使用有毒试剂, 可以便捷地用于制备较大量的BI-167107及结构相近的苯并噁嗪类化合物.

关键词： BI-167107; β2肾上腺素受体; 激动剂; GPCR; 苯并噁嗪; 合成

本文引用格式

王江波 , Seungkirl Ahn , Alem W.Kahsai , 刘蓉 , 任杰 , 胡昆 , 孙小强 , 陈新 . β2-AR激动剂BI-167107的合成[J]. 有机化学, 2013 , 33(03) : 634 -639 . DOI: 10.6023/cjoc201211015

Abstract

BI-167107 is a new long-acting β2-adrenergic receptor (β2-AR) agonist, and has important application in determining the critical structures of receptor/ligand proteins complex of G-protein-coupled receptor (GPCR). By employing 2-nitroresorcinol as starting material, a practical synthetic route for BI-167107 has been developed, involving 7-step reactions. The structure of the target molecule has been confirmed by 1H NMR, 13C NMR and MS techniques. The advantages of the synthetic route include avoiding use of toxic reagents and being suitable for scale up preparation of BI-167107 and other benzoxazine derivatives.

Key words： BI-167107; β2-adrenergic receptors; agonists; GPCR; benzoxazine; synthesis

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