Synthesis of Quinoxaline Derivatives as Intermediates to Obtain Erdafitinib

PHARMACEUTICAL CHEMISTRY JOURNAL(2021)

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摘要
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-1 H -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-1 H -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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关键词
quinoxaline derivatives, synthesis, triethylene diamine
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