反应条件
1: 90 percent / sodium carbonate / acetone / 18 h / Heating
2: 35 percent / nitric acid, acetic anhydride / 1) -20 deg C, 6 h; 2) room temperature, 4 h
3: H2 / Ni-raney / ethanol / 12 h / 50 °C
4: 84 percent / CH2Cl2 / 12 h / Heating
5: 93 percent / aq. NaOH / methanol / 18 h / Heating
6: 1.) aq. Cs2CO2 / 1) H2O, EtOH; 2) DMF, 40 deg C, overnight
7: TFA / CH2Cl2 / 1 h
8: 1.) dicyclohexylcarbodiimide, HOBt, 2.) TEA / 1) CH2Cl2, 1 h; 2) CH2Cl2, 2 h, 0 deg C, 20 deg C (15 h)
9: 95 percent / H2 / Pd/C / ethanol / 12 h
10: 59 percent / TFA, EDC / dimethylformamide / Ambient temperature
11: 77 percent / H2 / Pd/C / dimethylformamide / 6 h / Ambient temperature
View Scheme
参考文献
Bailly; Pommery; Houssin; Henichart
Journal of Pharmaceutical Sciences, 1989 , vol. 78, # 11 p. 910 - 917
