Water → HCID 66681066, compound

Participants

Reaction Conditions

Reaction Steps

N-{(2S)-2-hydroxy-3-[(triisopropylsilyl)oxy]propyl}-5-(3-[(1S)-2-methoxy-1-methylethoxy]-5-{[5-(methylsulfonyl)pyrazin-2-yl]oxy}phenyl)-1H-pyrrole-2-carboxamide (558 mg, 0.82 mmol) synthesized in Example (101b) was dissolved in tetrahydrofuran (20 mL), and anhydrous methanesulfonic acid (287 mg, 1.65 mmol) and triethylamine (0.34 mL, 2.47 mmol) were added, followed by stirring at 50° C. for 6 hours under nitrogen atmosphere. To the reaction solution, water (40 mL) was added, and extraction was carried out twice with methylene chloride (40 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: methanol/methylene chloride=0%-5%) to afford the desired compound (496 mg, yield 94%) as a white solid.

Provenance & Evidence