Improved procedure for the preparation of a rufinamide intermediate

摘要

Single step process for the preparation of the compound of formula 1H-I comprising 3H-I isomer in an amount less than about 0.2% of area measured by a chromatography method comprising: a) reaction of a compound of formula IX: where LG is a leaving group with sodium azide in the presence of a phase transfer catalyst and a non-polar solvent or a dipolar aprotic solvent with a boiling point below 100 ° C, b) reaction of the resulting mixture with a propiolic acid; and c) isolation of compound 1H-I.