Regioselective Radical Arylation of 3-Hydroxypyridines

J Org Chem. 2016 Jul 1;81(13):5752-8. doi: 10.1021/acs.joc.6b00894. Epub 2016 Jun 22.

Abstract

The titanium(III)-mediated radical arylation of 3-hydroxypyridines was found to proceed with high regioselectivity for the 2-position. Using aryldiazonium chlorides, which were prepared from the corresponding anilines, as aryl radical sources, a range of 3-hydroxy-2-phenylpyridines were obtained in moderate to good yields under simple reaction conditions. Reactions of ortho-carboxylic ester substituted phenyldiazonium salts directly provided tricyclic benzopyranopyridinones.

Publication types

  • Research Support, Non-U.S. Gov't