1: 2,4-di-Nitrobenzene With potassium borohydride in tetrahydrofuran; water Reduction; 2: formaldehyd; benzylamine in tetrahydrofuran; water Cycloaddition; Mannich reaction;
1.1: imidazole / acetonitrile / 3.17 h / 0 - 20 °C 1.2: 64 percent / acetonitrile / 20 - 50 °C 2.1: yellow HgO; sulfur / ethanol / 2 h / Heating View Scheme
参考文献
Scheffer, Ute; Strick, Andreas; Ludwig, Verena; Peter, Sascha; Kalden, Elisabeth; Goebel, Michael W.
Journal of the American Chemical Society, 2005 , vol. 127, # 7 p. 2211 - 2217
Coxon, Geoffrey D.; Furman, Brian L.; Harvey, Alan L.; McTavish, John; Mooney, Mark H.; Arastoo, Mahmoud; Kennedy, Alan R.; Tettey, Justice M.; Waigh, Roger D.
Journal of Medicinal Chemistry, 2009 , vol. 52, # 11 p. 3457 - 3463
1: benzylamine With hydrogenchloride in 1,4-dioxane; toluene 2: With dimethylaluminum chloride in 1,4-dioxane; toluene 0.5 h; 3: phenylacetonitrile in 1,4-dioxane; toluene T=80°C; 2 h;
