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Chinese Journal of Organic Chemistry >

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

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

Notes

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).

Fold

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

Cite this article

Wang Jiangbo , Ahn Seungkirl , Kahsai Alem W. , Liu Rong , Ren Jie , Hu Kun , Sun Xiaoqiang , Chen Xin . Synthesis of β2-AR Agonist BI-167107[J]. Chinese Journal of Organic Chemistry, 2013 , 33(03) : 634 -639 . DOI: 10.6023/cjoc201211015

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