1-BOC-4-(2-吡啶甲基)哌嗪合成路线 (共 5 条)
反应条件
hydrogenchloride; water in 1,4-dioxane; dichloromethane T=20°C; 5 h;
参考文献
Dong, Ming-Xin; Lu, Lu; Li, Haitao; Wang, Xiaohua; Lu, Hong; Jiang, Shibo; Dai, Qiu-Yun
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 9 p. 3284 - 3286
反应条件
1: piperazine-1-carboxylic acid tert-butyl ester With sodium hydride in N,N-dimethyl-formamide; mineral oil
T=0°C; 0.25 h; Inert atmosphere;
2: 2-pyridinylmethyl bromide in N,N-dimethyl-formamide; mineral oil
T=20°C; 4 h;
参考文献
MERCK SHARP and DOHME CORP.; MORRIELLO, Gregori, J.; WENDT, Harvey, R.; EDMONDSON, Scott, D.
Patent: WO2012/12314 A1, 2012 ;
Location in patent: Page/Page column 57 ;
WO 2012/012314 A1
反应条件
sodium hydroxide in tetrahydrofuran
24 h; Ambient temperature;
参考文献
Carceller, Elena; Merlos, Manuel; Giral, Marta; Almansa, Carmen; Bartroli, Javier; et al.
Journal of Medicinal Chemistry, 1993 , vol. 36, # 20 p. 2984 - 2997
反应条件
sodium tris(acetoxy)borohydride in dichloromethane; 1,2-dichloro-ethane
T=20°C; 20 h;
参考文献
Hoveyda, Hamid R.; Roy, Marie-Odile; Blanc, Sebastien; Noel, Sophie; Salvino, Joseph M.; Ator, Mark A.; Fraser, Graeme
Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 7 p. 1991 - 1996
反应条件
1: 88 percent / H2O / 18 h / Ambient temperature
2: 98 percent / 1.5 N aq. NaOH / tetrahydrofuran / 24 h / Ambient temperature
View Scheme
参考文献
Carceller, Elena; Merlos, Manuel; Giral, Marta; Almansa, Carmen; Bartroli, Javier; et al.
Journal of Medicinal Chemistry, 1993 , vol. 36, # 20 p. 2984 - 2997