Hydrochloric Acid → HCID 86707387, compound

Participants

Reaction Steps

To a solution of 4-({(4-acetylisoquinolin-3-yl)[4-(trifluoromethoxy)benzyl]amino}-sulfonyl)benzoic acid (20.0 mg, 0.036 mmol) prepared in Example 112 in ethanol (1 mL) was added sodium borohydride (10.0 mg, 0.264 mmol), and the mixture was stirred at room temperature for 3 hours. To the reaction solution was added 1 mol/L hydrochloric acid. The reaction solution was concentrated under reduced pressure, and then diluted with ethyl acetate, washed with water and saturated brine, dried over anhydrous sodium sulfate, and then concentrated under reduced pressure. The resulting residue was purified by silica gel column chromatography (chloroform:methanol=10:0→9:1) to give 4-({[4-(1-hydroxyethyl)isoquinolin-3-yl][4-(trifluoromethoxy)benzyl]amino}sulfonyl)benzoic acid (17.1 mg, 87%) as a white powder.

Provenance & Evidence