(1-Methyl-3-trifluoromethyl-1H-pyrazol-5-yl)-methanol synthesis

Yield:949898-58-2 58%

Reaction Conditions:

with borane-THF in tetrahydrofuran at 20; for 3 h;

Steps:

15.1 Step 1: l-Methyl-3-(trifluoromethyl)-lH-pyrazol-5-yl] methanol

Step 1: l-Methyl-3-(trifluoromethyl)-lH-pyrazol-5-yl] methanol Borane (1M in THF; 9.0 mL, 9.0 mmol) was added to a solution of l-methyl-5- (trifluoromethyl)pyrazole-3-carboxylic acid (350 mg, 1.8 mmol) in THF (10 mL) at rt. The mixture was stirred was stirred for 3 hours. It was then cooled to 0 °C and quenched with water. The mixture was extracted with EtOAc (3x) and the combined organic layers were washed with brine, dried over Na₂SC>4, filtered, and concentrated. The residue was purified on silica gel to afford [l-methyl-3-(trifluoromethyl)- lH-pyrazol-5-yi]methanol (188 mg; 58%) as a colorless oil. LCMS (FA): m/z = 18l (M+H).

References:

WO2015/2994,2015,A2 Location in patent:Paragraph 00187