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[4-AMINO-2-(TRIFLUOROMETHYL)PYRIMIDIN-5-YL]METHANOL synthesis

2synthesis methods
-

Yield:1514-01-8 95.8%

Reaction Conditions:

with lithium aluminium tetrahydride in tetrahydrofuran at 0; for 1 h;Inert atmosphere;

Steps:

1.3 Step 3:

To a solution of intermediate 3 (235 mg, 0.990 mmol) in THF (5 mL) were added LiAlH4 (94.0 mg, 2.49 mmol) at 0 °C and the mixture was stirred at 0 °C for 1 hour. The mixture was quenched with H2O/aq NaOH (15%)/ H2O (1/1/3). The mixture was extracted with EtOAc and washed with brine, dried over anhydrous Na2SO4, filtered and concentrated to dryness to give intermediate 4 (185 mg, yield 95.8%) as a white solid. The crude product was used to next step directly. LC/MS (ESI) (m/z): 194 (M+H)+.

References:

WO2021/168320,2021,A1 Location in patent:Paragraph 112; 186-187

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