(S)-1-N-Boc-2-甲基哌嗪合成路线 (共 10 条)
反应条件
1: (S)-(+)-2-Methylpiperazine With n-butyllithium in tetrahydrofuran T=20°C; 0.5 h; 2: With tert-butyldimethylsilyl chloride in tetrahydrofuran 1 h; 3: di-tert-butyl dicarbonate in tetrahydrofuran 1 h;
参考文献
GLAXO GROUP LIMITED
Patent: WO2006/55553 A2, 2006 ;
Location in patent: Page/Page column 36; 37 ;
WO 2006/055553 A2
反应条件
hydrogen; palladium 10 on activated carbon in methanol
参考文献
MILLENNIUM PHARMACEUTICALS, INC.
Patent: WO2005/66139 A2, 2005 ;
Location in patent: Page/Page column 134 ;
WO 2005/066139 A2
反应条件
hydrogen; palladium dihydroxide in ethanol Ambient temperature;
参考文献
Mickelson, John W.; Belonga, Kenneth L.; Jacobsen, Jon E.
Journal of Organic Chemistry, 1995 , vol. 60, # 13 p. 4177 - 4183
反应条件
hydrogenchloride in ethanol; water 1.5 h;
参考文献
WO2006/56752 A1, ;
Page/Page column 90 ;
WO 2006/056752 A1
反应条件
1: 99 percent / triethylamine / CH2Cl2 / 20 h / 20 °C 2: hydrogen; acetic acid / palladium on carbon / methanol / 24 h / 20 °C / 760 Torr View Scheme
参考文献
Synthetic Communications, , vol. 34, # 22 p. 4111 - 4118
反应条件
1: 85 percent / LAH / tetrahydrofuran / Heating 2: 94 percent / CH2Cl2 / Ambient temperature 3: 97 percent / H2 / Pd(OH)2 / ethanol / Ambient temperature View Scheme
参考文献
Journal of Organic Chemistry, , vol. 60, # 13 p. 4177 - 4183
反应条件
1: TFA / CH2Cl2 / 0 °C 2: DEAD, PPh3 / tetrahydrofuran / Ambient temperature 3: 85 percent / LAH / tetrahydrofuran / Heating 4: 94 percent / CH2Cl2 / Ambient temperature 5: 97 percent / H2 / Pd(OH)2 / ethanol / Ambient temperature View Scheme
参考文献
Journal of Organic Chemistry, , vol. 60, # 13 p. 4177 - 4183
反应条件
1: triethylamine / methanol / 20 h / Heating 2: 79 percent / lithium aluminum hydride / tetrahydrofuran / 36 h / 0 - 20 °C 3: 99 percent / triethylamine / CH2Cl2 / 20 h / 20 °C 4: hydrogen; acetic acid / palladium on carbon / methanol / 24 h / 20 °C / 760 Torr View Scheme
参考文献
Synthetic Communications, , vol. 34, # 22 p. 4111 - 4118
反应条件
1: 79 percent / lithium aluminum hydride / tetrahydrofuran / 36 h / 0 - 20 °C 2: 99 percent / triethylamine / CH2Cl2 / 20 h / 20 °C 3: hydrogen; acetic acid / palladium on carbon / methanol / 24 h / 20 °C / 760 Torr View Scheme
参考文献
Synthetic Communications, , vol. 34, # 22 p. 4111 - 4118
反应条件
1.1: N-ethyl-N,N-diisopropylamine / dimethyl sulfoxide / 48 h / 120 °C
2.1: trifluoroacetic acid / dichloromethane / 20 °C
2.2: pH 8
View Scheme
参考文献
BIOENERGENIX; MCCALL, John M.; ROMERO, Donna L.; KELLY, Robert C.
Patent: WO2012/119046 A2, 2012 ;