反应详情

To a suspension of 0.10 g (0.31 mmol) 6-chloro-1-(3,5-difluoro-benzyl)-1H-indole-3-carboxylic acid and one drop of DMF in 2 ml dichloromethane were added dropwise at 0° C. 0.032 ml (0.37 mmol) oxalyl chloride. The mixture was allowed to warm to room temperature, stirred for 1 h and subsequently added dropwise to a solution of 74 mg (0.34 mmol) 1-piperidin-4-yl-1,3-dihydro-indol-2-one and 63 mg (0.62 mmol) triethylamine in 1 ml dichloromethane at room temperature. After stirring over night the reaction mixture was concentrated and the residue was purified by flash chromatography to give 78 mg (48%) of the title compound as a light yellow solid.

1. additionwere added dropwise at 0° C
2. stirringAfter stirring over night the reaction mixture
3. concentrationwas concentrated
4. customthe residue was purified by flash chromatography