1-Boc-4-氨基哌啶合成路线 （共 62 条）
反应条件
1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 60 °C
2: ammonium formate; palladium hydroxide on carbon / ethanol / 75 °C
3: triethylamine / tetrahydrofuran / 20 °C
View Scheme
参考文献
Pryde, David C.; Tran, Thien-Duc; Gardner, Iain; Bright, Helen; Stupple, Paul; Galan, Sebastien; Alsop, Liam; Watson, Lesa; Middleton, Donald S.; Dayal, Satish; Platts, Michelle; Murray, Edward J.; Parkinson, Tanya; Webster, Robert
Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 3 p. 827 - 833
反应条件
N-ethyl-N,N-diisopropylamine in 1-methyl-pyrrolidin-2-one
T=80 - 120°C;
参考文献
PFIZER INC.
Patent: WO2006/21886 A1, 2006 ;
Location in patent: Page/Page column 84 ;
WO 2006/021886 A1
反应条件
1: in ethanol
4 h; Heating / reflux;
2: With sodium tetrahydroborate in ethanol
T=20°C; 24 h;
3: With water in ethanol
参考文献
ILDONG PHARMACEUTICAL CO., LTD.
Patent: US2010/168421 A1, 2010 ;
Location in patent: Page/Page column 9 ;
反应条件
1: With titanium(IV) isopropylate in ethanol
T=0 - 20°C;
2: With sodium tetrahydroborate; acetic acid in ethanol
T=20°C; 3 h;
参考文献
VITAS PHARMA RESEARCH PVT LTD; ALAPATI, Chandrasekhar; BANERJEE, Ankita; RANGARAJAN, Radha; KUMAR, Rajinder
Patent: WO2014/57415 A2, 2014 ;
Location in patent: Page/Page column 25 ;
反应条件
1: 2) NaBH4 / 1) methanol, 20 deg C, 1 h; 2) 1 h
2: 78 percent / H2 / Pd/C / ethanol / 10 h / 20 °C / 2585.7 Torr
View Scheme
参考文献
Obase; Takai; Teranishi; Nakamizo
Journal of Heterocyclic Chemistry, 1983 , vol. 20, # 3 p. 565 - 573
反应条件
1: 78 percent / DIEA / dimethylformamide / 15 h / 70 °C
2: 75 percent / H2 / Pd/C / ethanol / 1 h
View Scheme
参考文献
PRINCIPIA BIOPHARMA INC.; BRAMELD, Kenneth, A.; OWENS, Tim, A.
Patent: WO2014/36016 A1, 2014 ;
反应条件
potassium carbonate in dimethyl sulfoxide
T=100°C; 12 h;
参考文献
ASTRAZENECA AB
Patent: WO2008/112440 A1, 2008 ;
Location in patent: Page/Page column 45 ;
WO 2008/112440 A1
反应条件
9,9-dimethyl-4,5-bis(diphenyl-phosphino)xanthene; sodium t-butanolate; tris-(dibenzylideneacetone)dipalladium(0) in 1,4-dioxane
T=100°C; 72 h;
参考文献
PROXIMAGEN LTD.; BOYD, Joe William; MEO, Paul; HIGGINBOTTOM, Michael; SIMPSON, Iain; MOUNTFORD, David Mark; SAVORY, Edward Daniel
Patent: WO2012/101453 A1, 2012 ;
Location in patent: Page/Page column 25 ;
WO 2012/101453 A1
反应条件
caesium carbonate; palladium diacetate; 2,2'-bis-(diphenylphosphino)-1,1'- binaphthyl in 1,4-dioxane
T=90°C; 16 h;
参考文献
ARES TRADING S.A.; JORAND-LEBRUN, Catherine; SWINNEN, Dominique; GERBER, Patrick; KULKARNI, Santosh
Patent: WO2012/130915 A1, 2012 ;
Location in patent: Page/Page column 60 ;
WO 2012/130915 A1
反应条件
copper(l) iodide; (α-isobutyryl)cyclohexanone; caesium carbonate in N,N-dimethyl-formamide
T=70°C;
参考文献
Foley, Timothy L.; Rai, Ganesha; Yasgar, Adam; Daniel, Thomas; Baker, Heather L.; Attene-Ramos, Matias; Kosa, Nicolas M.; Leister, William; Burkart, Michael D.; Jadhav, Ajit; Simeonov, Anton; Maloney, David J.
Journal of Medicinal Chemistry, 2014 , vol. 57, # 3 p. 1063 - 1078
