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4(3H)-Quinazolinone, 5-(trifluoromethyl)- synthesis

4synthesis methods
-

Yield:436-73-7 91%

Reaction Conditions:

in butan-1-ol at 100; for 5 h;

Steps:

1 Step 1: synthesis of 5 -(trifluoromethyl)quinazo lin-4(3H)-one 14-b

A mixture of 2-amino-6-(trifluoromethyl)benzoic acid 14-a (9.00 g, 43.9 mmol) and formamidine acetate (22.84 g, 219.4 mmol) in n-butanol (180 ml) was stirred at 100°C for5 hours. The solvent was evaporated under vacuum. The residue was washed with ethanol (2 x 50 ml) and then dried in vacuum at 45°C for 1 hour to give intermediate 14-b (9 g, yield:91%).

References:

WO2016/91791,2016,A1 Location in patent:Page/Page column 26