Acetic Acid → 7-[3-(tert-butyldimethylsilyloxy)propylamino]-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one

참여 물질

반응 단계

The 7-amino-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one (300 mg, 0.986 mmol) obtained in step C of Example 1-1 was dissolved in methanol (10 ml). Thereafter, 3-[(tert-butyldimethylsilyl)oxy]-1-propanol (186 mg, 0.986 mmol), acetic acid (0.339 ml), and a 1 M sodium cyanoborohydride THF solution (2.96 ml, 2.96 mmol) were added at 0° C. to the obtained solution, and the obtained mixture was stirred at a room temperature for 1 hour. Thereafter, a saturated sodium bicarbonate solution was added to the reaction mixture, and the obtained mixture was then extracted with methylene chloride. The extract was dried over magnesium sulfate, and was then concentrated under reduced pressure. The obtained residue was purified by silica gel chromatography (ethyl acetate:hexane=1:3), so as to obtain 7-[3-(tert-butyldimethylsilyloxy)propylamino]-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one (376 mg, 80%).

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