N-Boc-4-羟基哌啶合成路线 （共 171 条）
反应条件
1: 1-(tert-Butyloxycarbonyl)-4-piperidinol With sodium hydride in 1-methyl-pyrrolidin-2-one T=20°C; 0.166667 h; 2: 2-bromo-pyridine in 1-methyl-pyrrolidin-2-one 6 h; Heating / reflux;
参考文献
PFIZER LIMITED; PFIZER INC.
Patent: WO2005/105779 A1, 2005 ;
Location in patent: Page/Page column 38 ;
WO 2005/105779 A1
反应条件
18-crown-6 ether in toluene 18 h; Heating / reflux;
参考文献
PIRAMED LIMITED
Patent: WO2006/46031 A1, 2006 ;
Location in patent: Page/Page column 68 ;
WO 2006/046031 A1
反应条件
triphenylphosphine in tetrahydrofuran
参考文献
Shima, Ichiro; Ohkawa, Takehiko; Sato, Kentaro; Ishibashi, Naoki; Imamura, Kenichiro
Patent: US2004/97425 A1, 2004 ;
反应条件
1: 1-(tert-Butyloxycarbonyl)-4-piperidinol With sodium hydride in tetrahydrofuran T=0°C; 0.333333 h; 2: 2-chloro-5-nitro-pyridine in tetrahydrofuran T=0 - 22°C;
参考文献
ELI LILLY AND COMPANY
Patent: WO2007/53394 A1, 2007 ;
Location in patent: Page/Page column 20 ;
WO 2007/053394 A1
反应条件
diethyl azidocarboxylate; triphenylphosphine in tetrahydrofuran T=20°C;
参考文献
PFIZER PRODUCTS INC.
Patent: WO2004/9550 A1, 2004 ;
Location in patent: Page 47 ;
WO 2004/009550 A1
反应条件
1: 1-(tert-Butyloxycarbonyl)-4-piperidinol With sodium hydride in DMF (N,N-dimethyl-formamide) T=50°C; 0.75 h; 2: 4-fluorobenzenecarbonitrile in DMF (N,N-dimethyl-formamide) T=50°C; 2 h;
参考文献
ELI LILLY AND COMPANY
Patent: WO2005/61442 A1, 2005 ;
Location in patent: Page/Page column 44 ;
WO 2005/061442 A1
反应条件
sodium hydride in N,N-dimethyl-formamide T=65°C; 16 h;
参考文献
Dvorak, Curt A.; Apodaca, Richard; Barbier, Ann J.; Berridge, Craig W.; Wilson, Sandy J.; Boggs, Jamin D.; Xiao, Wei; Lovenberg, Timothy W.; Carruthers, Nicholas I.
Journal of Medicinal Chemistry, 2005 , vol. 48, # 6 p. 2229 - 2238
参考文献
Takeda Chemical Industries, Ltd.
Patent: US6562978 B1, 2003 ;
反应条件
1: 4-chloro pyridine hydrochloride With sodium hydride in dimethyl sulfoxide T=70°C; 0.916667 h; Inert atmosphere; 2: 1-(tert-Butyloxycarbonyl)-4-piperidinol in dimethyl sulfoxide T=20°C; Inert atmosphere;
参考文献
Bailey, James M.; Bruton, Gordon; Huxley, Anthony; Johnstone, Vicky; Milner, Peter H.; Orlek, Barry S.; Stemp, Geoffrey
Synlett, 2009 , # 7 p. 1051 - 1054
反应条件
potassium carbonate in dimethyl sulfoxide T=70°C; 3 h; Product distribution / selectivity;
参考文献
GLAXO GROUP LIMITED
Patent: WO2005/14571 A1, 2005 ;
Location in patent: Page/Page column 16 ;
WO 2005/014571 A1
