4-(1H-吲唑-5-基)哌啶-1-羧酸叔丁酯合成路线 (共 4 条)
反应条件
hydrogen; palladium on activated charcoal in methanol; water T=20°C; P=7500.75 Torr; 12 h;
参考文献
MERCK SERONO S.A.; JORAND-LEBRUN, Catherine; CROSIGNANI, Stefano; DORBAIS, Jerome; GRIPPI-VALLOTTON, Tania; PRETRE, Adeline
Patent: WO2012/84704 A1, 2012 ;
Location in patent: Page/Page column 118-119 ;
WO 2012/084704 A1
反应条件
1: 4-Iodo-piperidine-1-carboxylic acid,tert-butyl ester With chloro-trimethyl-silane; zinc in N,N-dimethyl acetamide; ethylene dibromide T=40 - 65°C; 0.666667 h; Inert atmosphere; 2: 5-bromo-1H-indazole With (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; copper(l) iodide in N,N-dimethyl acetamide; ethylene dibromide T=85°C; Inert atmosphere;
参考文献
3-V BIOSCIENCES, INC.; OSLOB, Johan D.; MCDOWELL, Robert S.; JOHNSON, Russell; YANG, Hanbiao; EVANCHIK, Marc; ZAHARIA, Cristiana A.; CAI, Haiying; HU, Lily W.
Patent: WO2014/8197 A1, 2014 ;
Location in patent: Page/Page column 130 ;
反应条件
1: potassium carbonate / 1,1'-bis-(diphenylphosphino)ferrocene / 1,4-dioxane; water / 24 h / 90 °C 2: hydrogen / palladium on activated charcoal / water; methanol / 12 h / 20 °C / 7500.75 Torr View Scheme
参考文献
MERCK SERONO S.A.; JORAND-LEBRUN, Catherine; CROSIGNANI, Stefano; DORBAIS, Jerome; GRIPPI-VALLOTTON, Tania; PRETRE, Adeline
Patent: WO2012/84704 A1, 2012 ;
WO 2012/084704 A1
反应条件
1: potassium carbonate / 1,1'-bis-(diphenylphosphino)ferrocene / 1,4-dioxane; water / 24 h / 90 °C 2: hydrogen / palladium on activated charcoal / water; methanol / 12 h / 20 °C / 7500.75 Torr View Scheme
参考文献
MERCK SERONO S.A.; JORAND-LEBRUN, Catherine; CROSIGNANI, Stefano; DORBAIS, Jerome; GRIPPI-VALLOTTON, Tania; PRETRE, Adeline
Patent: WO2012/84704 A1, 2012 ;
WO 2012/084704 A1