Hydrochloric Acid → HCID 66682539, compound

Participants

Reaction Steps

5-{3-[(1S)-2-Methoxy-1-methylethoxy]-5-[4-(methylsulfonyl)phenoxy]phenyl}-1H-pyrrole-2-carboxylic acid (250 mg, 0.561 mmol) synthesized in Example (18a) was dissolved in dichloromethane (10 mL), and 3-amino-1-propanol (90.04, 1.18 mmol), WSCI•HCl (165 mg, 0.861 mmol) and 4-dimethylaminopyridine (140 mg, 1.15 mmol) were added, followed by stirring at room temperature for 16 hours under nitrogen atmosphere. 1N hydrochloric acid (10 mL) was added, and the solution was separated with dichloromethane (15 mL). The organic layer was washed with saturated brine, and subsequently dried over anhydrous magnesium sulfate. The solvent was distilled off under reduced pressure, and the resulting residue was purified using silica gel column chromatography (elution solvent: ethyl acetate/hexane=60%-100%) to afford the desired product (216 mg, yield 77%) as a white solid.

Provenance & Evidence