Formic Acid → HCID 58765501, compound

Participants

Reaction Conditions

Reaction Steps

To formic acid (2.5 mL, 65 mmol) at 0° C. was added acetic anhydride (500 μL, 5.2 mmol) and the mixture was stirred at 0° C. for 10 minutes. This was added to a solution of 1-{[(4S)-2-(hydroxyamino)-4-phenylpentyl]sulfonyl}-4-[4-(phenylethynyl)phenyl]piperazine (345 mg, 0.685 mmol) in CH2Cl2 (5 mL) cooled to 0° C. The reaction was brought to RT and stirred for one hour. Volatiles were then removed in vacuo. The residue was then precipitated in MeOH (10 mL) and heated to 40° C. for two hours, dissolving. The solution was then cooled to RT and concentrated in vacuo. The residue was then purified by flash chromatography (silica gel, 1–2% MeOH in CH2Cl2) to give the title compound as a white foam (330 mg, 0.621 mmol, 91%).

Provenance & Evidence