Facile synthesis of halogenated spiroketals via a tandem iodocyclization

Org Lett. 2014 Apr 18;16(8):2236-9. doi: 10.1021/ol500741a. Epub 2014 Apr 4.

Abstract

A strategy for the synthesis of spiroketal compounds through a tandem iodocyclization of 1-(2-ethynylphenyl)-4-hydroxybut-2-yn-1-one derivatives is presented. This reaction could proceed under very mild conditions in a short time and avoid the use of expensive and toxic metal catalysts. Moreover, the resulting halides can be further exploited by subsequent palladium-catalyzed coupling reactions, which act as the important intermediates for building other valuable compounds.