反应条件
1: 68 percent / NaOH / methanol; H2O / 2.5 h / 20 °C 2: H2 / Pd/C / dimethylformamide / 2 h / 23 °C 3: Cs2CO3 / dimethylformamide / 2 h / 100 °C 4: 56 percent / Cs2CO3 / dimethylformamide / 3 h / 23 °C 5: TFA / CH2Cl2 / 4 h / 23 °C 6: 87 percent / CH2Cl2 / 1 h / 23 °C 7: 82 percent / HCl / dioxane / 1 h / 23 °C 8: 98 percent / pyridine / CH2Cl2 / 1 h / 0 °C 9: 88 percent / diisopropylethylamine; dimethylaminopyridine / acetonitrile / 6 h / 40 °C 10: 83 percent / Zn; AcOH / H2O / 7 h / 23 °C 11: 50 percent / NaNO2; AcOH / tetrahydrofuran; H2O / 3 h / 0 °C 12: 95 percent / EDC*HCl; DMAP / CH2Cl2 / 3 h / 23 °C 13: 90 percent / Bu3SnH; AcOH / (PPh3)2PdCl2 / CH2Cl2 / 0.25 h / 23 °C 14: 91 percent / benzeneseleninic anhydride / CH2Cl2 / 0.08 h / -10 °C 15: 58 percent View Scheme
参考文献
Pharma Mar, S.A.; Martín López, Ma Jesús; Francesch Solloso, Andrés; Cuevas Marchante, Maria del Carmen
Patent: US2013/66067 A1, 2013 ;