反应详情

The mixture 3-[(2-Amino-ethyl)-(2,2-dimethyl-propyl)-amino]-6-chloro-3-(3-chloro-benzyl)-1,3-dihydro-indol-2-one (75 mg, 0.179 mmol), 4-Acetyl-piperazine-1-carbonyl chloride (41 mg, 0.215 mmol) and K2CO3 (37 mg, 0.268 mmol) in dichloro-methane (2 mL) was stirred at room temperature for 2 h. Then the solution was concentrated and the crude product was purified by chromatography to give 42 mg rac-4-Acetyl-piperazine-1-carboxylic acid{2-[[6-chloro-3-(3-chloro-benzyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-(2,2-dimethyl-propyl)-amino]-ethyl}-amide of as a yellow solid. Then 15 mg rac-4-Acetyl-piperazine-1-carboxylic acid{2-[[6-chloro-3-(3-chloro-benzyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-(2,2-dimethyl-propyl)-amino]-ethyl}-amide was separated by chiral column to obtain 4 mg 4-Acetyl-piperazine-1-carboxylic acid{2-[[(S)-6-chloro-3-(3-chloro-benzyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-(2,2-dimethyl-propyl)-amino]-ethyl}-amide

1. concentrationThen the solution was concentrated
2. customthe crude product was purified by chromatography