反应详情

1,8-Diazabicyclo[5.4.0]undec-7-ene (0.12 ml) was added to 4-bromo-N-cyclopropyl-2-fluoro-N′-hydroxybenzenecarboximidamide (Intermediate 52) (0.2 g) in tetrahydrofuran (2 ml) then heated at 150° in a microwave for 70 min. The mixture was applied to a Varian Bond-Elut SPE cartridge (silica, 20 g) then eluted with cyclohexane:ethyl acetate (100:0 to 80:20) to give the title compound as a white solid (0.13 g).

1. temperaturethen heated at 150° in a microwave for 70 min
2. washthen eluted with cyclohexane:ethyl acetate (100:0 to 80:20)