Facile assembly of fused benzo[4,5]furo heterocycles

被引:85
作者
Liu, Jing [1 ]
Fitzgerald, Anne E. [1 ]
Mani, Neelakandha S. [1 ]
机构
[1] Johnson & Johnson Pharmaceut Res & Dev LLC, San Diego, CA 92121 USA
关键词
D O I
10.1021/jo8000595
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A concise synthesis of fused benzo[4,5]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 benzo[4,5]furo heterocycles.
引用
收藏
页码:2951 / 2954
页数:4
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