(S)-1-((R)-2-甲氧基-1-(4-(三氟甲基)苯基)乙基)-2-甲基-4-(4-甲基哌啶-4-基)哌嗪合成路线 (共 8 条)
反应条件
trifluoroacetic acid in dichloromethane
T=20°C; 6 h;
参考文献
Tagat, Jayaram R.; McCombie, Stuart W.; Nazareno, Dennis; Labroli, Marc A.; Xiao, Yushi; Steensma, Ruo W.; Strizki, Julie M.; Baroudy, Bahige M.; Cox, Kathleen; Lachowicz, Jean; Varty, Geoffrey; Watkins, Robert
Journal of Medicinal Chemistry, 2004 , vol. 47, # 10 p. 2405 - 2408
反应条件
1.1: borane dimethylsulfide; (S)-2-methyl-CBS-oxaborolidine / 1 h
2.1: triethylamine / CH2Cl2 / 0.5 h / cooling
3.1: 14.8 g / K2CO3 / acetonitrile / 72 h / Heating
4.1: 7.9 g / trifluoroacetic acid / CH2Cl2 / 3 h / 20 °C
5.1: Ti(OiPr)4 / CH2Cl2 / 20 h / 20 °C
5.2: 13.4 g / CH2Cl2; toluene / 20 h
6.1: 76 percent / tetrahydrofuran / 48 h / 20 °C
7.1: 100 percent / trifluoroacetic acid / CH2Cl2 / 6 h / 20 °C
View Scheme
参考文献
Tagat, Jayaram R.; McCombie, Stuart W.; Nazareno, Dennis; Labroli, Marc A.; Xiao, Yushi; Steensma, Ruo W.; Strizki, Julie M.; Baroudy, Bahige M.; Cox, Kathleen; Lachowicz, Jean; Varty, Geoffrey; Watkins, Robert
Journal of Medicinal Chemistry, 2004 , vol. 47, # 10 p. 2405 - 2408
反应条件
1.1: Ti(OiPr)4 / CH2Cl2 / 20 h / 20 °C
1.2: 13.4 g / CH2Cl2; toluene / 20 h
2.1: 76 percent / tetrahydrofuran / 48 h / 20 °C
3.1: 100 percent / trifluoroacetic acid / CH2Cl2 / 6 h / 20 °C
View Scheme
参考文献
Tagat, Jayaram R.; McCombie, Stuart W.; Nazareno, Dennis; Labroli, Marc A.; Xiao, Yushi; Steensma, Ruo W.; Strizki, Julie M.; Baroudy, Bahige M.; Cox, Kathleen; Lachowicz, Jean; Varty, Geoffrey; Watkins, Robert
Journal of Medicinal Chemistry, 2004 , vol. 47, # 10 p. 2405 - 2408
反应条件
1.1: triethylamine / CH2Cl2 / 0.5 h / cooling
2.1: 14.8 g / K2CO3 / acetonitrile / 72 h / Heating
3.1: 7.9 g / trifluoroacetic acid / CH2Cl2 / 3 h / 20 °C
4.1: Ti(OiPr)4 / CH2Cl2 / 20 h / 20 °C
4.2: 13.4 g / CH2Cl2; toluene / 20 h
5.1: 76 percent / tetrahydrofuran / 48 h / 20 °C
6.1: 100 percent / trifluoroacetic acid / CH2Cl2 / 6 h / 20 °C
View Scheme
参考文献
Tagat, Jayaram R.; McCombie, Stuart W.; Nazareno, Dennis; Labroli, Marc A.; Xiao, Yushi; Steensma, Ruo W.; Strizki, Julie M.; Baroudy, Bahige M.; Cox, Kathleen; Lachowicz, Jean; Varty, Geoffrey; Watkins, Robert
Journal of Medicinal Chemistry, 2004 , vol. 47, # 10 p. 2405 - 2408
反应条件
1.1: 14.8 g / K2CO3 / acetonitrile / 72 h / Heating
2.1: 7.9 g / trifluoroacetic acid / CH2Cl2 / 3 h / 20 °C
3.1: Ti(OiPr)4 / CH2Cl2 / 20 h / 20 °C
3.2: 13.4 g / CH2Cl2; toluene / 20 h
4.1: 76 percent / tetrahydrofuran / 48 h / 20 °C
5.1: 100 percent / trifluoroacetic acid / CH2Cl2 / 6 h / 20 °C
View Scheme
参考文献
Tagat, Jayaram R.; McCombie, Stuart W.; Nazareno, Dennis; Labroli, Marc A.; Xiao, Yushi; Steensma, Ruo W.; Strizki, Julie M.; Baroudy, Bahige M.; Cox, Kathleen; Lachowicz, Jean; Varty, Geoffrey; Watkins, Robert
Journal of Medicinal Chemistry, 2004 , vol. 47, # 10 p. 2405 - 2408
反应条件
1.1: Ti(OiPr)4 / CH2Cl2 / 20 h / 20 °C
1.2: 13.4 g / CH2Cl2; toluene / 20 h
2.1: 76 percent / tetrahydrofuran / 48 h / 20 °C
3.1: 100 percent / trifluoroacetic acid / CH2Cl2 / 6 h / 20 °C
View Scheme
参考文献
Tagat, Jayaram R.; McCombie, Stuart W.; Nazareno, Dennis; Labroli, Marc A.; Xiao, Yushi; Steensma, Ruo W.; Strizki, Julie M.; Baroudy, Bahige M.; Cox, Kathleen; Lachowicz, Jean; Varty, Geoffrey; Watkins, Robert
Journal of Medicinal Chemistry, 2004 , vol. 47, # 10 p. 2405 - 2408
反应条件
1.1: 7.9 g / trifluoroacetic acid / CH2Cl2 / 3 h / 20 °C
2.1: Ti(OiPr)4 / CH2Cl2 / 20 h / 20 °C
2.2: 13.4 g / CH2Cl2; toluene / 20 h
3.1: 76 percent / tetrahydrofuran / 48 h / 20 °C
4.1: 100 percent / trifluoroacetic acid / CH2Cl2 / 6 h / 20 °C
View Scheme
参考文献
Tagat, Jayaram R.; McCombie, Stuart W.; Nazareno, Dennis; Labroli, Marc A.; Xiao, Yushi; Steensma, Ruo W.; Strizki, Julie M.; Baroudy, Bahige M.; Cox, Kathleen; Lachowicz, Jean; Varty, Geoffrey; Watkins, Robert
Journal of Medicinal Chemistry, 2004 , vol. 47, # 10 p. 2405 - 2408
反应条件
1: 76 percent / tetrahydrofuran / 48 h / 20 °C
2: 100 percent / trifluoroacetic acid / CH2Cl2 / 6 h / 20 °C
View Scheme
参考文献
Tagat, Jayaram R.; McCombie, Stuart W.; Nazareno, Dennis; Labroli, Marc A.; Xiao, Yushi; Steensma, Ruo W.; Strizki, Julie M.; Baroudy, Bahige M.; Cox, Kathleen; Lachowicz, Jean; Varty, Geoffrey; Watkins, Robert
Journal of Medicinal Chemistry, 2004 , vol. 47, # 10 p. 2405 - 2408