Phosphine oxide-catalyzed enantioselective intramolecular aldol reaction via regioselective enolization of unsymmetrical diketones with tetrachlorosilane

Org Lett. 2014 Sep 19;16(18):4802-5. doi: 10.1021/ol502269w. Epub 2014 Sep 5.

Abstract

The phosphine oxide-catalyzed asymmetric intramolecular aldol reactions of diketones were investigated. The combination of tetrachlorosilane and a chiral phosphine oxide catalyst promoted the acetyl-selective enolization of diketones, and the subsequent intramolecular aldol reaction occurred in an enantioselective manner. The introduction of two trimethylsilyl groups at the 4- and 4'-positions in BINAP dioxide catalyst improved the enantioselectivity. This reaction provides an effective synthetic method to access β-tertiary-hydroxy cyclohexanones in high yields and with high enantioselectivity.

Publication types

  • Research Support, Non-U.S. Gov't