2-[[4-[(2,4-二氨基蝶啶-6-基)甲基-甲基氨基]苯甲酰基]氨基]-5-[(2-甲基丙烷-2-基)氧基]-5-氧代戊酸合成路线 （共 14 条）
反应条件
barium dihydroxide in ethanol; water
Ambient temperature;
参考文献
Rosowsky, Andre; Forsch, Ronald; Uren, Jack; Wick, Michael
Journal of Medicinal Chemistry, 1981 , vol. 24, # 12 p. 1450 - 1455
反应条件
1: 100 percent / cesium carbonate / dimethylformamide / Ambient temperature
2: 85 percent / H2, AcOH / 5percent Pd/C / methanol / 2280 - 3040 Torr
3: 1.) diethyl phosphorocyanidate, Et3N, 2.) Et3N / 1.) DMF, 80 deg C, 2 min, 2.) DMF, 80 deg C, 2 h
4: 92 percent / Ba(OH)2*8H2O / ethanol; H2O / Ambient temperature
View Scheme
参考文献
Rosowsky, Andre; Forsch, Ronald; Uren, Jack; Wick, Michael
Journal of Medicinal Chemistry, 1981 , vol. 24, # 12 p. 1450 - 1455
反应条件
1: 85 percent / H2, AcOH / 5percent Pd/C / methanol / 2280 - 3040 Torr
2: 1.) diethyl phosphorocyanidate, Et3N, 2.) Et3N / 1.) DMF, 80 deg C, 2 min, 2.) DMF, 80 deg C, 2 h
3: 92 percent / Ba(OH)2*8H2O / ethanol; H2O / Ambient temperature
View Scheme
参考文献
Rosowsky, Andre; Forsch, Ronald; Uren, Jack; Wick, Michael
Journal of Medicinal Chemistry, 1981 , vol. 24, # 12 p. 1450 - 1455
反应条件
N-ethyl-N,N-diisopropylamine in N,N-dimethyl acetamide
T=45 - 50°C; 25 h; Yield given;
参考文献
Rosowsky; Freisheim; Bader; Forsch; Susten; Cucchi
Journal of Medicinal Chemistry, 1985 , vol. 28, # 5 p. 660 - 667
反应条件
1: 1.) diethyl phosphorocyanidate, Et3N, 2.) Et3N / 1.) DMF, 25 deg C, 2.5 h, 2.) DMF, 25 deg C, 70 h
2: 86 percent / aq. Ba(OH)2 / 22 h
View Scheme
参考文献
Rosowsky; Freisheim; Bader; Forsch; Susten; Cucchi
Journal of Medicinal Chemistry, 1985 , vol. 28, # 5 p. 660 - 667
反应条件
1: Br2, triphenylphosphine / N,N-dimethyl-acetamide / 18 h / 25 °C
2: i-Pr2NEt / N,N-dimethyl-acetamide / 25 h / 45 - 50 °C
View Scheme
参考文献
Rosowsky; Freisheim; Bader; Forsch; Susten; Cucchi
Journal of Medicinal Chemistry, 1985 , vol. 28, # 5 p. 660 - 667
反应条件
1: 84 percent / CHCl3 / 3 h / 20 °C
2: 94 percent / SOCl2 / 0.75 h / Heating
3: 100 percent / Et3N / CH2Cl2 / 17 h / Ambient temperature
4: 100 percent / aq. NaOH / ethanol / 2.5 h / 20 °C
5: i-Pr2NEt / N,N-dimethyl-acetamide / 25 h / 45 - 50 °C
View Scheme
参考文献
Rosowsky; Freisheim; Bader; Forsch; Susten; Cucchi
Journal of Medicinal Chemistry, 1985 , vol. 28, # 5 p. 660 - 667
反应条件
1: 100 percent / Et3N / CH2Cl2 / 17 h / Ambient temperature
2: 100 percent / aq. NaOH / ethanol / 2.5 h / 20 °C
3: i-Pr2NEt / N,N-dimethyl-acetamide / 25 h / 45 - 50 °C
View Scheme
参考文献
Rosowsky; Freisheim; Bader; Forsch; Susten; Cucchi
Journal of Medicinal Chemistry, 1985 , vol. 28, # 5 p. 660 - 667
反应条件
1: 94 percent / SOCl2 / 0.75 h / Heating
2: 100 percent / Et3N / CH2Cl2 / 17 h / Ambient temperature
3: 100 percent / aq. NaOH / ethanol / 2.5 h / 20 °C
4: i-Pr2NEt / N,N-dimethyl-acetamide / 25 h / 45 - 50 °C
View Scheme
参考文献
Rosowsky; Freisheim; Bader; Forsch; Susten; Cucchi
Journal of Medicinal Chemistry, 1985 , vol. 28, # 5 p. 660 - 667
反应条件
1: 100 percent / aq. NaOH / ethanol / 2.5 h / 20 °C
2: i-Pr2NEt / N,N-dimethyl-acetamide / 25 h / 45 - 50 °C
View Scheme
参考文献
Rosowsky; Freisheim; Bader; Forsch; Susten; Cucchi
Journal of Medicinal Chemistry, 1985 , vol. 28, # 5 p. 660 - 667
