Facile assembly of fused benzo[4,5]furo heterocycles |
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Authors: | Liu Jing Fitzgerald Anne E Mani Neelakandha S |
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Institution: | Johnson & Johnson Pharmaceutical Research & Development, LLC, 3210 Merryfield Row, San Diego, CA 92121, USA. jliu30@prdus.jnj.com |
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Abstract: | A concise synthesis of fused benzo4,5]furo heterocycles 18 has been developed. Chemo/regioselective Suzuki coupling between 1,2-dihaloarene 17 and alpha-hydroxyphenylboronic acid or ester 20 gives biaryl phenol 19, which then undergoes copper(I) thiophene-2-carboxylate (CuTC)-mediated intramolecular cyclization to afford 18 in good overall yield. This method has broad substrate scope and allows facile assembly of a wide variety of benzo4,5]furo heterocycles. |
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