Trifluoroacetic acid → 3-((S)-5-Pyrrolidin-2-yl-pyridin-3-yl)-1H-indole

Participants

Reaction Steps

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.

Provenance & Evidence