3,3,3-Trifluoropropane-1-sulfonyl chloride → 3,3,3-Trifluoropropane-1-sulfonic acid 4-[1-(2,4-dichlorophenyl)-3-methyl-4-oxo-5-piperidin-1-yl-4,5-dihydro-1H-pyrrolo[3,2-c]pyridin-2-yl]phenyl ester

Participants

Reaction Steps

3,3,3-Trifluoro-propane-1-sulfonyl chloride (100 mg, 0.509 mmol) was added to 1-(2,4-dichlorophenyl)-2-(4-hydroxyphenyl)-3-methyl-5-piperidin-1-yl-1,5-dihydro-4H-pyrrolo[3,2-c]pyridin-4-one (74 mg, 0.158 mmol) dissolved in pyridine (5 ml) at 0° C. The reaction was continued at 0° C. for 1 h and 15 min and then at rt. After 15 min at rt more 3,3,3-trifluoro-propane-1-sulfonyl chloride (260 mg, 1.323 mmol) was added. After 15 min the solvent was evaporated. Purified by flash chromatography (20-100% EtOAc in toluene) to yield the title compound as a white solid after evaporation (24 mg, 24%).

Provenance & Evidence