反应详情

温度

120 °C

1-Cyclobutyl-4-(4-piperidinylmethyl)piperidine (may be prepared as described in Description 6) (0.15 g), 5-bromo-2-trifluoromethylpyrimidine (may be prepared as described in F. Cottet and M. Schlosser, Eur. J. Org. Chem., 2002, 327) (0.129 g), tris(dibenzylidineacetone)dipalladium(0) (0.053 g), 2-dicyclohexylphosphino-2′-(N,N-dimethylamino)biphenyl (0.088 g) and sodium tert-butoxide (0.092 g) were added to dioxane (2 ml) and heated at 120° C. for 14 min in the microwave reactor. The crude reaction mixture was passed through an SCX column (10 g, eluting with methanol [80 ml ] then 2 N NH3 in methanol [80 ml]). Chromatography (silica gel, eluting with methanol/dichloromethane, 0-20%) afforded the title compound (E35) (0.08 g). MS electrospray (+ion) 383 (MH+).

1. customThe crude reaction mixture
2. washeluting with methanol [80 ml ]
3. washChromatography (silica gel, eluting with methanol/dichloromethane, 0-20%)