反应详情

Reaction of intermediate 22, ethyl 1,2-dimethyl-7-hydroxy-3,6-dioxo-2,3,4,6-tetrahydro-1H-pyrimido[2,1-c][1,2,4]triazine-8-carboxylate, (0.050 g, 0.177 mmol) with 3,4-dichlorobenzylamine (0.10 g, 0.57 mmol) as described in the preparation of example 1 gave 0.054 g (74% yield) of the title amide as a white solid. 1HNMR 400 MHz (CDCl3) δ (ppm): 3.28 (3H, s, NCH3), 3.32 (3H, s, NCH3), 4.59 (2H, d, J=6.7 Hz, NCH2), 4.68 (2H, s, CH2), 7.21 (1H, dd, J=2.0 Hz and J=8.0 Hz, aromatic), 7.44 (1H, d, J=2.0 Hz, aromatic), 7.46 (1H, d, J=8.0 Hz, aromatic), 7.78 (1H, broad t, NH), 11.85 (1H, s, OH). MS (ESI+) m/z 413 [M+H+].

1. customas described in the preparation of example 1