反应条件
1: 1.) oxalyl chloride, DMSO, 2.) triethylamine / 1.) CH2Cl2, -78 deg C, 0.5 h, 2.) CH2Cl2, -70 deg C, 2 h 2: 55 percent / VCl3*(THF)3, Zn / CH2Cl2 3: 91 percent / diisopropylethylamine / dimethylformamide / 48 h / 50 °C 4: 52 percent / H2 / 10percent Pd/C / ethyl acetate; methanol 5: 1.) NaH / 1.) DMF, 15 min, 2.) DMF, a) 0 deg C, 15 min, b) RT, 2 h 6: HCl / methanol; dioxane View Scheme
参考文献
Lam, Patrick Y. S.; Ru, Yu; Jadhav, Prabhakar K.; Aldrich, Paul E.; DeLucca, George V.; Eyermann, Charles J.; Chang, Chong-Hwan; Emmett, George; Holler, Edward R.; Daneker, Wayne F.; Li, Liangzhu; Confalone, Pat N.; McHugh, Robert J.; Han, Qi; Li, Renhua; Markwalder, Jay A.; Seitz, Steven P.; Sharpe, Thomas R.; Bacheler, Lee T.; Rayner, Marlene M.; Klabe, Ronald M.; Shum, Linyee; Winslow, Dean L.; Kornhauser, David M.; Jackson, David A.; Erickson-Viitanen, Susan; Hodge, C. Nicholas
Journal of Medicinal Chemistry, 1996 , vol. 39, # 18 p. 3514 - 3525
