Acetic Acid → 7-tetrazol-1-yl-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one

Participants

Reaction Conditions

Reaction Steps

17.5 μl (0.16 mmol) of trimethyl orthoformate and 9.8 mg (0.15 mmol) of sodium azide were added to 0.2 ml of an acetic acid solution containing the 7-amino-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one obtained in Example 38. The obtained mixture was stirred at 80° C. for 6 hours. Thereafter, the reaction solution was cooled to a room temperature, and water was then added to thereto, followed by extraction with ethyl acetate. The extract was washed with a saturated sodium bicarbonate aqueous solution, and was then dried over anhydrous sodium sulfate, followed by concentration. The obtained residue was purified by silica gel column chromatography (ethyl acetate:hexane=2:1), so as to obtain 29.8 mg (83%) of 7-tetrazol-1-yl-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one in the form of a colorless solid.

Provenance & Evidence