Sodium Hydroxide → Pemafibrate

Participants

Reaction Steps

n-Butyl (R)-2-[3-[N-(benzoxazol-2-yl)-N-(3-(4-methoxyphenoxy)propyl)aminomethyl]phenoxyl]butyrate (68 mg) was dissolved in ethanol (2 mL), and a 4 N aqueous sodium hydroxide solution (0.2 mL) was added at 0° C. Then, the resulting mixture was stirred at room temperature for 3 hours. Ethanol was distilled off, and water was added, and then the reaction liquor was acidified with concentrated hydrochloric acid in an ice-cold bath. The reaction liquor was extracted with ethyl acetate, and the extract was washed with water and saturated brine, and dried over dry sodium sulfate. The solution was filtered and concentrated under reduced pressure, and then the residue was purified by silica gel column chromatography (chloroform/methanol=10/1) to obtain a colorless solid (60 mg, 100%).

Provenance & Evidence