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Synthesis of Quinoxaline Derivatives as Intermediates to Obtain Erdafitinib

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Pharmaceutical Chemistry Journal Aims and scope

As an important member of multi-nitrogen heterocyclic compounds, quinoxalines have various biological activities which are widely used in chemistry, biomedicine and chemical industry. In this work, quinoxaline derivative 7-bromo-2-(1-methyl-1H-pyrazol-4-yl)quinoxaline (5), which is an essential intermediate to obtain drug Erdafitinib, has been synthesized in reasonably good yield using 4-bromobenzene-1,2-diamine (4) and 2-bromo-1-(1-methyl-1H-pyrazol-4-yl)ethan-1-one (3) as raw materials, triethylene diamine (DABCO) as catalyst, and tetrahydrofuran as solvent. To the best of our knowledge, this is the first time compound 5 has been acquired by the proposed method.

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Acknowledgments

The project was funded by the key laboratory of marine bioactive substances and modern analysis technology, SOA (MBSMAT-2017-06)

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Authors and Affiliations

  1. College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao, 266042, P. R. China

    Xiaohua Sun, Lijun Feng, Chuance Sun & Congmin Kang

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  1. Xiaohua Sun
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  2. Lijun Feng
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  3. Chuance Sun
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  4. Congmin Kang
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Correspondence to Congmin Kang.

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Sun, X., Feng, L., Sun, C. et al. Synthesis of Quinoxaline Derivatives as Intermediates to Obtain Erdafitinib. Pharm Chem J 55, 951–953 (2021). https://doi.org/10.1007/s11094-021-02521-x

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  • DOI: https://doi.org/10.1007/s11094-021-02521-x

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