反应详情

温度

120 °C

2-Chloromethyl-6-(4-ethoxy-3-trifluoromethyl-phenyl)-1H-imidazo[4,5-c]pyridine-4-carbonitrile (20 mg, 0.053 mmol) was dissolved in DMF and N-methyl piperazine (26 mg, 0.26 mmol) was added. The mixture was heated to 120° C. for five minutes in a Smith Creator microwave. Mixture was diluted with methanol (4 ml) and loaded onto an SCX cartridge. Cartridge was washed three times with methanol (5 ml) then eluted with 2M methanolic ammonia. Methanolic ammonia was removed by evaporation under reduced pressure then mixture was prep HPLC purified to afford 8 mg of 6-(4-ethoxy-3-trifluoromethyl-phenyl)-2-(4-methyl-piperazin-1-ylmethyl)-1H-imidazo[4,5-c]pyridine-4-carbonitrile as a white solid. 1H NMR (MeOH) δ 8.28-8.20 (m, 2H), 8.13 (s, 1H), 7.26 (d, 1H), 4.22 (q, 2H), 3.92 (s, 2H), 2,67 (m, 8H), 2.38 (s, 3H), 1.45 (t, 3H). MS m/z 445.5 (M+1).

1. washCartridge was washed three times with methanol (5 ml)
2. washthen eluted with 2M methanolic ammonia
3. customMethanolic ammonia was removed by evaporation under reduced pressure
4. custompurified