1-Hydroxybenzotriazole → 5-[5-(2,6-Dichloro-phenylmethanesulfonyl)-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid [2-(3-Acetylamino-pyrrolidin-1-yl)-ethyl]-amide

Participants

Reaction Steps

To a solution of 5-[5-(2,6-dichloro-phenylmethanesulfonyl)-2-oxo-1,2-dihydro-indol-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (252 mg, 0.5 mmol) in DMF (10 mL) was added HOBt (101 mg, 1.5 eq.), EDAC.HCl (144 mg, 1.5 eq.) and TEA (152 mg, 3 eq.). After stirring at rf 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 30° C. for 72 hours, the reaction was concentrated and the residue was purified on a silica gel column to give 213 mg (65%) of the titled compound as an orange solid.

Provenance & Evidence