反应详情

Reaction of intermediate 13, ethyl 6-hydroxy-1-methyl-2,5-dioxo-1,2,3,5-tetrahydroimidazo[1,2-a]pyrimidine-7-carboxylate (0.070 g, 0.28 mmol) with 3,4-dimethylbenzylamine (0.15 g, 1.12 mmol) as described in the preparation of example 1 gave 0.042 g (58% yield) of the title amide as a white solid. 1HNMR 400 MHz (DMSO-d6) δ (ppm): 2.18 (3H, s, CH3), 2.20 (3H, s, CH3), 3.14 (3H, s, NCH3), 4.42 (2H, d, J=6.3 Hz, NCH2), 4.47 (2H, s, CH2), 7.0–7.1 (3H, m, aromatics), 9.40 (1H, broad t, NH), 12.35 (1H, s, OH). MS (ESI+) m/z 343 [M+H+].

1. customas described in the preparation of example 1