反应详情

A solution of 3-(5-{(S)-1-[1-(4-Methoxy-phenyl)-ethyl]-pyrrolidin-2-yl}-pyridin-3-yl)-indole-1-carboxylic acid tert-butyl ester 5 (300 mg, 0.63 mmole) in 4 mL of TFA was heated at 100° C. in a microwave reactor for 20 minutes. The result solution was concentrated to remove TFA as much as possible. The residue was purified by HPLC (Column: Waters Sunfire, 30×30 mm; Mobile phase: CH3CN 15% H2O 85% with 0.1% TFA to CH3CN 60% H2O 40% with 0.1% TFA by gradient in 11 minutes; Flow rate 45 mL/minute; Detector: 215 nm UV) to give 3-((S)-5-Pyrrolidin-2-yl-pyridin-3-yl)-1H-indole 6 (78 mg, yield 49%) as white solid.

1. concentrationThe result solution was concentrated
2. customto remove TFA as much as possible
3. customThe residue was purified by HPLC (Column: Waters Sunfire, 30×30 mm; Mobile phase: CH3CN 15% H2O 85% with 0.1% TFA to CH3CN 60% H2O 40% with 0.1% TFA by gradient in 11 minutes; Flow rate 45 mL/minute; Detector: 215 nm UV)