反应条件
1: 90 percent / DMAP / 3 h / 80 °C 2: 90 percent / pyridine / dimethylformamide / 2 h / 20 °C 3: 0.230 g / methanol; tetrahydrofuran / 26 h / 20 °C 4: 76 percent / 48percent aq. HBr / 7 h / 120 °C 5: 98 percent / DMAP; Et3N / CH2Cl2 / 0.5 h / 20 °C 6: 51 percent / NBS; dibenzoyl peroxide / CCl4 / 3.83 h / 85 °C / Irradiation 7: 73 percent / 2,6-lutidine / dimethylformamide / 5.5 h / 120 °C 8: 80 percent / aq. NaOH / tetrahydrofuran / 1 h / 20 °C 9: 94 percent / Et3N / CH2Cl2 / 0.92 h 10: 77 percent / CH2Cl2 / 2.5 h / 20 °C 11: 0.142 g / TFA / CH2Cl2 / 0.92 h / 20 °C 12: PyBOP; diisopropylethylamine / dimethylformamide / 3 h View Scheme
参考文献
Bavetsias; Skelton; Yafai; Mitchell; Wilson; Allan; Jackman
Journal of Medicinal Chemistry, 2002 , vol. 45, # 17 p. 3692 - 3702