Cesium carbonate → 6-(N'-tert-Butoxycarbonylhydrazino)-2-(2-chlorophenylamino)-3,4-difluorobenzoic acid methyl ester

Participants

Reaction Steps

Pd2(dba)3 (4 mol %), t-butylcarbazate (4.00 equivalents), dppf (12 mol %) and Cs2CO3 (1.00 equivalent) are added to a solution of 6-bromo-2-(2-chlorophenylamino)-3,4-difluorobenzoic acid methyl ester (1.00 equivalent) in PhMe. The reaction mixture is heated in a sealed vial charged under a N2 atmosphere to 100° C. and stirred for 16 hours. After cooling to room temperature, the reaction mixture is diluted with methylene chloride and filtered. The filtrate is concentrated under reduced pressure. The product is purified by trituration or flash column chromatography if further purification is necessary.

Provenance & Evidence