反应详情

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.

1. temperatureThe reaction mixture is heated in a sealed
2. additionvial charged under a N2 atmosphere to 100° C.
3. filtrationfiltered
4. concentrationThe filtrate is concentrated under reduced pressure
5. customThe product is purified by trituration or flash column chromatography if further purification