反应详情

A mixture of 1-oxo-3-(4-trifluoromethyl-phenyl)-1,2-dihydro-pyrrolo[1,2-a]pyrazine-6-carbonitrile (Example 2), (0.05 g, 0.16 mmol), hydroxylamine hydrochloride (15 mg, 0.22 mmol) and N,N-diisopropylethylamine (86.4 μL, 0.49 mmol,) was stirred in methylene chloride (0.5 mL), methanol (0.5 mL) and N,N-dimethylformamide (0.2 mL) at 45° C. for 2 d. At this time, the resulting solids were collected by filtration to afford N-hydroxy-1-oxo-3-(4-trifluoromethyl-phenyl)-1,2-dihydro-pyrrolo[1,2-a]pyrazine-6-carboxamidine (40 mg, 70%) as an off-white solid. 1H NMR (methanol-d4) δ ppm 7.83 (q, J=8.4 Hz, 4H), 7.73 (s, 2H), 7.37 (s, 1H). LC-MS calcd. for C15H12F3N4O2 [(M+H)+] 337, obsd. 337.0.

1. filtrationAt this time, the resulting solids were collected by filtration