1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → 3-[1-(4-{(S)-2-[(Cyclopropylmethyl-amino)-methyl]-pyrrolidine 1-carbonyl}-3,5-dimethyl-1H-pyrrol-2-yl)-meth-(Z)-ylidene]-5-(2,6-dichloro-phenylmethanesulfonyl)-1,3-dihydro-indol-2-one

Participants

Reaction Steps

To a mixture of 5-[5-(2,6-dichloro-phenylmethanesulfonyl)-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (100 mg, 0.2 mmol), EDAC (76 mg), HOBt (27 mg) in DMF (4 mL) was added cyclopropylmethyl-(S)-1-pyrrolidin-2-ylmethyl-amine (0.05 mL) and TEA (0.08 mL). The mixture was stirred at rt for 2 days. The reaction was concentrated and the residue was purified on a silica gel column to give the titled compound.

Provenance & Evidence