1-Boc-4-氨基哌啶合成路线 （共 62 条）
反应条件
1: triethylamine / dichloromethane / 16 h / 20 °C 2: 10 palladium on activated charcoal; ammonia; hydrogen / methanol / 20 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 19, # 16 p. 4935 - 4952
反应条件
in dichloromethane T=0 - 23°C; 2 h;
参考文献
US2011/92475 A1, ;
Page/Page column 17 ;
反应条件
1.1: N-chloro-succinimide / toluene / 0.33 h / Inert atmosphere 2.1: titanium(IV) isopropylate / tetrahydrofuran; toluene / 0.08 h / -40 °C / Inert atmosphere 2.2: 4 h / -40 - 20 °C / Inert atmosphere View Scheme
参考文献
Barker, Timothy J.; Jarvo, Elizabeth R.
Angewandte Chemie - International Edition, 2011 , vol. 50, # 36 p. 8325 - 8328
反应条件
triethylamine in dichloromethane T=20°C; 72 h;
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; NEUROCRINE BIOSCIENCES, INC.; TRAN, Joe, A.; CHEN, Chen
Patent: WO2010/149685 A1, 2010 ;
Location in patent: Page/Page column 49 ;
WO 2010/149685 A1
反应条件
1: 1-t-butoxycarbonyl-4-aminopiperidine; α-bromoacetophenone With N-ethyl-N,N-diisopropylamine in dichloromethane T=20°C; 17 h; 2: cyanic acid sodium salt With acetic acid in dichloromethane T=0 - 20°C; pH=4; 16 h;
参考文献
Gutierrez, Corey; Termin, Andreas; Hadida-Ruah, Sara; Joshi, Pramod; Bergeron, Daniele; Yoo, Sanghee; Binch, Hayley; Come, Jon; Cao, Jingrong; Nanthakumar, Suganthi
Patent: US2008/4261 A1, 2008 ;
Location in patent: Page/Page column 137 ;
US 20080004261 A1
参考文献
Dr. Karl Thomae GmbH
Patent: US6344/449 B1, 2002 ;
Location in patent: Example A1a) ;
Title/Abstract Full Text Show Details
Dr. Karl Thomae GmbH
Patent: US6344449 B1, 2002 ;
Location in patent: Example A1a) ;
反应条件
1: With sodium acetate; acetic acid in tetrahydrofuran T=20°C; 3 h; 2: With sodium tris(acetoxy)borohydride in tetrahydrofuran T=20°C; 16 h; 3: With water in tert-butyl methyl ether
参考文献
SOLVAY PHARMACEUTICALS GmbH
Patent: US2007/149512 A1, 2007 ;
Location in patent: Page/Page column 17 ;
反应条件
N-ethyl-N,N-diisopropylamine in isopropyl alcohol 48 h; Heating / reflux;
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG
Patent: WO2007/106705 A1, 2007 ;
Location in patent: Page/Page column 102 ;
WO 2007/106705 A1
反应条件
1: With acetic acid in methanol 0.25 h; 2: With sodium cyanoborohydride in methanol T=20°C; 0.5 h;
参考文献
SOLVAY PHARMACEUTICALS GmbH
Patent: US2007/149512 A1, 2007 ;
Location in patent: Page/Page column 15-16 ;
反应条件
sodium cyanoborohydride; acetic acid in acetonitrile T=20°C; 16 h;
参考文献
Nazare, Marc; Essrich, Melanie; Will, David William; Matter, Hans; Ritter, Kurt; Wehner, Volkmar
Patent: US2003/199689 A1, 2003 ;
Location in patent: Page/Page column 33 ;
