Methylamine → 5-Amino-1-(4-fluorophenyl)-N-{3,3,3-trifluoro-2-hydroxy-2-[(methylamino)methyl]propyl}-1H-pyrazole-4-carboxamide

Participants

Reaction Conditions

Reaction Steps

To a solution of 5-amino-1-(4-fluorophenyl)-N-{[2-(trifluoromethyl)-2-oxiranyl]methyl}-1H-pyrazole-4-carboxamide (750 mg, 2.18 mmol) in anhydrous tetrahydrofuran (10 ml) was added methylamine (2M in tetrahydrofuran, 4 ml, 8 mmol) and stirred at 21° C. for 15 hours. It was evaporated to give a foam which was triturated with diethyl ether (ca. 5 ml). The resulting solid was filtered off and washed with a little diethyl ether and then petroleum ether)(40-60° to give the title compound (465 mg).

Provenance & Evidence