反应详情

温度

55 °C

7-(1-Methyl-1H-pyrazol-4-yl)-5-(1H-pyrazol-4-yl)imidazo[1,2-c]pyrimidine (Preparation K; 0.165 g, 0.622 mmol) was suspended in CH3CN (5 mL) and (E)-dimethyl pent-2-enedioate (0.295 g, 1.87 mmol) was added followed by DBU (0.0947 g, 0.622 mmol). The reaction was warmed to 55° C. and heated for 9 hours. The reaction was then cooled and concentrated. The residue was purified on silica gel (1-4% methanol in DCM) to afford dimethyl 3-(4-(7-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-c]pyrimidin-5-yl)-1H-pyrazol-1-yl)pentanedioate (205 mg, 78% yield). MS (apci) m/z=424.2 (M+H).

1. temperatureheated for 9 hours
2. temperatureThe reaction was then cooled
3. concentrationconcentrated
4. customThe residue was purified on silica gel (1-4% methanol in DCM)