反应详情

温度

100 °C

The 5-[2-(2-bromo-phenyl)-acetylamino]-4′-methyl-biphenyl-3-carboxylic acid methyl ester from step 1 was dissolved in toluene (3 mL) and CsCO3 (325 mg, 1 equive.), Pd(OAc)2 (15 mg) and XANTPHOS (59 mg) were added. The reaction mixture was stirred overnight at 100° C., then cooled and partitioned between water and ethyl acetate. The organic layer was separated and concentrated under reduced pressure, and the residue was purified by preparative thin layer chromatography (2:1 hexanes:ethyl acetate) to give 4′-methyl-5-(2-oxo-2,3-dihydro-indol-1-yl)-biphenyl-3-carboxylic acid methyl ester, which was used directly in the next step.

1. temperaturecooled
2. custompartitioned between water and ethyl acetate
3. customThe organic layer was separated
4. concentrationconcentrated under reduced pressure
5. customthe residue was purified by preparative thin layer chromatography (2:1 hexanes:ethyl acetate)