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4-(DIFLUOROMETHYL)BENZOIC ACID synthesis

7synthesis methods
-

Yield: 98%

Reaction Conditions:

with lithium hydroxide monohydrate;water in tetrahydrofuran at 20; for 3 h;Inert atmosphere;

Steps:

34.B
[00227] Step B: A mixture of methyl 4-(difluoromethyl)benzoate (1.1 g, 5.9 mmol) and LiOH H20 (1.24 g, 29.5 mmol) in THF/H20 (30/10 mL) was stirred at room temperature for 3 hours. The mixture was acidified by IN HC1 to a pH of 2 and extracted with EtOAc. The organic layer was washed with water and brine, dried over Na2S04, filtered and concentrated to give 4-(difluoromethyl)benzoic acid (1.0 g, 98.0% yield).

References:

ARRAY BIOPHARMA INC.;GENENTECH, INC.;HICKEN, Erik James;HUNT, Kevin W.;RODRIGUEZ, Martha E.;TANG, Tony P.;SIU, Michael WO2013/148851, 2013, A1 Location in patent:Paragraph 00227

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