反应详情

温度

20 °C

To a solution of 3-((S)-5-Pyrrolidin-2-yl-pyridin-3-yl)-1H-indole 6 (78 mg, 0.30 mmole) and (S)-[(S)-2-(tert-Butoxycarbonyl-methyl-amino)-propionylamino]-cyclohexyl-acetic acid (111.6 mg, 0.33 mmole) in 5 ml of THF at 0° C., was added 4-(4,6-Dimethoxy-[1,3,5]triazin-2-yl)-4-methyl-morpholinium chloride hydrate (98.6 mg, 0.36 mmole) in one portion. After stirring at 20° C. for 2 hours, the reaction mixture was diluted with 30 mL of EtOAc, washed with 3×10 mL of water and concentration to give [(S)-1-(S)-1-Cyclohexyl-2-{(S)-2-[5-(1H-indol-3-yl)-pyridin-3-yl]-pyrrolidin-1-yl}-2-oxo-ethylcarbamoyl)-ethyl]-methyl-carbamic acid tert-butyl ester 7 (143.5 mg, crude) as pale yellow solid without further purification for next step.

1. washwashed with 3×10 mL of water and concentration