反应详情

A solution of 3-Bromo-5-{(S)-1-[(R)-1-(4-methoxy-phenyl)-ethyl]-pyrrolidin-2-yl}-pyridine 3 (3.64 g, 10.0 mmole) in 5 mL of TFA was heated at 120° C. in a microwave reactor for 30 minutes. The resulting solution was concentrated to remove TFA. The residue was dissolved in 150 mL of CH2Cl2 and basicfied by 5 mL of saturated NaHCO3. The solution was washed by 2×10 mL of water, dried over Na2SO4 and concentrated to give 3-((S)-5-Pyrrolidin-2-yl-pyridin-3-yl)-1H-indole 4 (2.4 g, crude) as deep brown gum without further purification for the next step reaction.

1. concentrationThe resulting solution was concentrated
2. customto remove TFA
3. dissolutionThe residue was dissolved in 150 mL of CH2Cl2
4. washThe solution was washed by 2×10 mL of water
5. dry with materialdried over Na2SO4
6. concentrationconcentrated