N-[[(1R,2S,3S,4R)-2,3-二(2-氨基-3H-咪唑-4-基)-4-[[(4-溴1h-吡咯-2-羰基)氨基]甲基]环丁基]甲基]-4-溴-1H-吡咯-2-甲酰胺二盐酸盐合成路线 （共 6 条）
反应条件
1: TsOH / methanol / 24 h / 50 °C
2: diisobutylaluminum hydride / CH2Cl2 / 1 h / -78 °C
3: pyridine / 1 h / 0 - 20 °C
4: sodium azide / dimethylformamide / 24 h / 50 °C
5: p-toluenesulfonic acid / methanol / 24 h / 50 °C
6: H2 / Lindlar catalyst / methanol / 12 h / 23 °C / 760 Torr
7: acetonitrile / 4 h
8: benzyltrimethylammonium dichloroiodate / tetrahydrofuran / 1.75 h / 60 °C
9: acetonitrile / 40 h / 35 °C
10: aq. HCl / methanol / 16 h / 23 °C
11: H2O / 4 h / 95 °C
View Scheme
参考文献
O'Malley, Daniel P.; Li, Ke; Maue, Michael; Zografos, Alexandros L.; Baran, Phil S.
Journal of the American Chemical Society, 2007 , vol. 129, # 15 p. 4762 - 4775
反应条件
1: pyridine / 1 h / 0 - 20 °C
2: sodium azide / dimethylformamide / 24 h / 50 °C
3: p-toluenesulfonic acid / methanol / 24 h / 50 °C
4: H2 / Lindlar catalyst / methanol / 12 h / 23 °C / 760 Torr
5: acetonitrile / 4 h
6: benzyltrimethylammonium dichloroiodate / tetrahydrofuran / 1.75 h / 60 °C
7: acetonitrile / 40 h / 35 °C
8: aq. HCl / methanol / 16 h / 23 °C
9: H2O / 4 h / 95 °C
View Scheme
参考文献
O'Malley, Daniel P.; Li, Ke; Maue, Michael; Zografos, Alexandros L.; Baran, Phil S.
Journal of the American Chemical Society, 2007 , vol. 129, # 15 p. 4762 - 4775
反应条件
1: p-toluenesulfonic acid / methanol / 24 h / 50 °C
2: H2 / Lindlar catalyst / methanol / 12 h / 23 °C / 760 Torr
3: acetonitrile / 4 h
4: benzyltrimethylammonium dichloroiodate / tetrahydrofuran / 1.75 h / 60 °C
5: acetonitrile / 40 h / 35 °C
6: aq. HCl / methanol / 16 h / 23 °C
7: H2O / 4 h / 95 °C
View Scheme
参考文献
O'Malley, Daniel P.; Li, Ke; Maue, Michael; Zografos, Alexandros L.; Baran, Phil S.
Journal of the American Chemical Society, 2007 , vol. 129, # 15 p. 4762 - 4775
反应条件
1: p-toluenesulfonic acid / toluene / 12 h / 105 °C
2: TsOH / methanol / 24 h / 50 °C
3: diisobutylaluminum hydride / CH2Cl2 / 1 h / -78 °C
4: pyridine / 1 h / 0 - 20 °C
5: sodium azide / dimethylformamide / 24 h / 50 °C
6: p-toluenesulfonic acid / methanol / 24 h / 50 °C
7: H2 / Lindlar catalyst / methanol / 12 h / 23 °C / 760 Torr
8: acetonitrile / 4 h
9: benzyltrimethylammonium dichloroiodate / tetrahydrofuran / 1.75 h / 60 °C
10: acetonitrile / 40 h / 35 °C
11: aq. HCl / methanol / 16 h / 23 °C
12: H2O / 4 h / 95 °C
View Scheme
参考文献
O'Malley, Daniel P.; Li, Ke; Maue, Michael; Zografos, Alexandros L.; Baran, Phil S.
Journal of the American Chemical Society, 2007 , vol. 129, # 15 p. 4762 - 4775
参考文献
Keifer, Paul A.; Schwartz, Robert E.; Koker, Moustapha E. S.; Hughes, Robert G.; Rittschof, Dan; Rinehart, Kenneth L.
Journal of Organic Chemistry, 1991 , vol. 56, # 9 p. 2965 - 2975
反应条件
in water
T=95°C; 4 h;
参考文献
O'Malley, Daniel P.; Li, Ke; Maue, Michael; Zografos, Alexandros L.; Baran, Phil S.
Journal of the American Chemical Society, 2007 , vol. 129, # 15 p. 4762 - 4775
