反应详情

To a solution of {5-[5-(2,6-dichloro-phenylmethanesulfonyl)-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrol-3-yl}-acetic acid (260 mg, 0.5 mmol) in DMF (3 mL) was added HOBt (101 mg, 1.5 eq.), EDAC.HCl (144 mg, 3 eq.) and TEA (152 mg, 1.5 eq.). After stirring at rt for 30 mins, to the mixture was added N-[1-(2-amino-ethyl)-pyrrolidin-3-yl]-acetamide (128 mg, 1.5 eq.). After stirring at 40° C. for overnight, the cooled reaction was concentrated and the residue was purified on a silica gel column to give the title compound as a yellow solid.

1. stirringAfter stirring at 40° C. for overnight
2. customthe cooled reaction
3. concentrationwas concentrated
4. customthe residue was purified on a silica gel column