N-Boc-4-羟基哌啶合成路线 （共 171 条）
反应条件
1: triethylamine / dichloromethane / 3 h / 0 - 20 °C 2: sodium hydride / N,N-dimethyl-formamide; mineral oil / 12 h / 80 °C View Scheme
反应条件
1: triphenylphosphine; diethylazodicarboxylate / tetrahydrofuran / 25 h / 0 - 70 °C 2: trifluoroacetic acid / dichloromethane / 24 h / 20 °C View Scheme
参考文献
PIERRE FABRE MEDICAMENT; Leroy, Isabelle; Dupont-Passelaigue, Elisabeth; Mialhe, Samuel; Junquero, Didier; Valeille, Karine
Patent: US2013/40928 A1, 2013 ;
反应条件
triphenylphosphine; diethylazodicarboxylate in tetrahydrofuran T=0°C; Inert atmosphere;
参考文献
KADMON CORPORATION, LLC; BOXER, Michael; RYAN, John; TONRA, James
Patent: WO2014/55999 A2, 2014 ;
Location in patent: Paragraph 0238 ;
反应条件
1: triethylamine / dichloromethane / 0 - 20 °C / Inert atmosphere 2: sodium hydride / N,N-dimethyl-formamide; mineral oil / 0.5 h / 110 °C / Inert atmosphere; Microwave irradiation 3: dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct; potassium acetate / dimethyl sulfoxide / 3 h / 80 °C / Inert atmosphere View Scheme
参考文献
De Koning, Pieter D.; McAndrew, Douglas; Moore, Robert; Moses, Ian B.; Boyles, David C.; Kissick, Kyle; Stanchina, Corey L.; Cuthbertson, Timothy; Kamatani, Asayuki; Rahman, Leera; Rodriguez, Rick; Urbina, Armando; Sandovalnee Accacia, Alison; Rose, Peter R.
Organic Process Research and Development, 2011 , vol. 15, # 5 p. 1018 - 1026
反应条件
1.1: 1H-imidazole / N,N-dimethyl-formamide / 67 h / 40 °C 2.1: N,N,N',N,-tetramethylethylenediamine; sec.-butyllithium / diethyl ether; hexane / 4 h / -80 - -20 °C 2.2: -80 - 20 °C 3.1: tetra-n-butylammonium fluoride trihydrate / tetrahydrofuran / 12 h / 20 °C View Scheme
参考文献
Zeitschrift fur Naturforschung - Section B Journal of Chemical Sciences, , vol. 67, # 4 p. 373 - 388
反应条件
[Ni0(1,5-cyclooctadiene)2]; potassium tert-butylate; 1,3-bis(2,6-diisopropylphenyl)imidazolinium chloride in 2,4-dichlorotoluene T=25°C; 0.5 h; Inert atmosphere;
参考文献
Berini, Christophe; Winkelmann, Ole H.; Otten, Jennifer; Vicic, David A.; Navarro, Oscar
Chemistry - A European Journal, 2010 , vol. 16, # 23 p. 6857 - 6860
反应条件
1: triethylamine / dichloromethane / 2.17 h / 0 - 20 °C 2: methanol / 15 h / Reflux 3: hydrogenchloride / 1,4-dioxane; methanol / 0.03 h / Reflux View Scheme
参考文献
EXELIXIS, INC.; RICE, Kenneth
Patent: WO2012/71509 A2, 2012 ;
WO 2012/071509 A2
反应条件
1.1: triphenylphosphine; di-isopropyl azodicarboxylate / tetrahydrofuran / 0.5 h / 0 °C 1.2: 16 h / 20 °C 2.1: methylhydrazine / dichloromethane / 16 h / 0 - 20 °C View Scheme
参考文献
LG LIFE SCIENCES LTD.; KIM, Young Kwan; JOO, Hyun Woo; KIM, Myoung Yeol; PARK, Heui Sul; LEE, Tae Hee; KWAK, Hyo Shin; SHIM, Dong Sup; CHOI, Eun Sil
Patent: WO2012/111995 A1, 2012 ;
WO 2012/111995 A1
反应条件
4,4'-diaminostilbene-2,2'-disulfonic acid in dichloromethane T=0°C; 1.5 h;
参考文献
Journal of Medicinal Chemistry, , vol. 47, # 11 p. 2906 - 2916
反应条件
1: triethylamine / dichloromethane / 8 h / 20 °C 2: 1,8-diazabicyclo[5.4.0]undec-7-ene / N,N-dimethyl-formamide / 150 °C View Scheme
