2-Fluorobenzylamine → HCID 58166437, compound

Participants

Reaction Steps

A solution of 5-fluoro-1-isobutyl-4-(1H-1,2,4-triazol-1-yl)pyrimidin-2(1H)-one (500 mg, 2.1 mmol) and 2-fluorobenzylamine (313 mg, 2.5 mmol) in dry 1,4-dioxane (10 mL) was heated to reflux for 1 h under nitrogen. After cooling to room temperature, the reaction mixture was concentrated in vacuo. Recrystallization from EtOAc/methyl tert-butylether afforded 5-fluoro-4-(2-fluorobenzylamino)-1-isobutylpyrimidin-2(1H)-one (545 mg, 89%) as an off white solid: mp 118-119° C.; 1H NMR (400 MHz, CDCl3) δ 7.45 (td, J=7.6, 1.7 Hz, 1H), 7.35-7.28 (m, 2H), 7.13 (ddd, J=21.9, 13.9, 7.3 Hz, 3H), 5.58 (s, 1H), 4.81 (d, J=5.4 Hz, 2H), 3.56 (d, J=7.5 Hz, 2H), 2.16 (dt, J=13.6, 6.8 Hz, 1H), 0.95 (d, J=6.7 Hz, 6H); ESIMS m/z 295 ([M+H]+).

Provenance & Evidence