Catalytic and asymmetric fluorolactonisations of carboxylic acids through anion phase transfer

Chemistry. 2014 Jan 3;20(1):83-6. doi: 10.1002/chem.201303385. Epub 2013 Dec 4.

Abstract

Catalytic fluorolactonisations of aromatic carboxylic acids have been developed. The reactions proceed under mild conditions using the commercially available reagent Selectfluor. A weak phase transfer of the reagent mediated by Na2CO3 allows the reaction to be conducted in non-polar solvents. Furthermore, by the use of a catalytic amount of (DHQ)2PHAL (hydroquinine 1,4-phthalazinediyl diether), the first asymmetric fluorolactonisation has been achieved. The corresponding isobenzofuran core can be found in many biologically active molecules.

Keywords: asymmetric synthesis; carboxylic acids; cyclisation; fluorination; lactones.