3-乙酰基-4-氧代-1-哌啶羧酸-1,1-二甲基乙酯合成路线 （共 10 条）
反应条件
ammonium chloride; diisopropylamine in tetrahydrofuran; ethyl acetate
参考文献
SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Jiancun; ZHANG, Yingjun; ZHANG, Weihong; LIU, Bing; ZHANG, Jiquan; LIU, Jinlei; ZHANG, Lu
Patent: WO2013/71697 A1, 2013 ;
Location in patent: Paragraph 00305 ;
反应条件
1: tert-butyl 4-oxo-piperidine-1-carboxylate With pyrrolidine in toluene 3 h; Inert atmosphereReflux; 2: acetic anhydride in 1,4-dioxane; toluene T=20°C; Inert atmosphere; 3: With water in 1,4-dioxane; toluene 1 h; Reflux; Product distribution / selectivity;
参考文献
GLAXO GROUP LIMITED; BAILEY, James, Matthew; BROWN, John, Alexander; DEMONT, Emmanuel, Hubert; SEAL, Gail, Astra, Lorraine; SMETHURST, Christian, Alan, Paul; WITHERINGTON, Jason; HARRISON, Lee, Andrew
Patent: WO2010/146104 A1, 2010 ;
Location in patent: Page/Page column 28-29 ;
WO 2010/146104 A1
反应条件
1: With triethylamine in dichloromethane T=0°C; 3 h; Inert atmosphere; 2: With water in dichloromethane 1 h; Inert atmosphere;
参考文献
Yogeeswari, Perumal; Sharma, Monika; Samala, Ganesh; Gangadhar, Matharasala; Karthick, Srirama; Mallipeddi, Saketh; Semwal, Arvind; Sriram, Dharmarajan
European Journal of Medicinal Chemistry, 2013 , vol. 66, p. 211 - 220
反应条件
sodium hydride in tetrahydrofuran; toluene T=40°C; 6 h;
参考文献
Wang, Pu-Sheng; Zhou, Xiao-Le; Gong, Liu-Zhu
Organic Letters, 2014 , vol. 16, # 3 p. 976 - 979
反应条件
1: tert-butyl 4-oxo-piperidine-1-carboxylate With lithium diisopropyl amide in tetrahydrofuran T=-78°C; 2 h; 2: 1-acetyl-1H-imidazole in tetrahydrofuran T=-78 - 20°C; 3: With ammonium chloride in tetrahydrofuran; water
参考文献
ACTELION PHARMACEUTICALS LTD.
Patent: WO2005/23781 A1, 2005 ;
Location in patent: Page/Page column 37 ;
WO 2005/023781 A1
反应条件
1.1: sodium carbonate / tetrahydrofuran; water / 0 - 20 °C 2.1: Dess-Martin periodane / dichloromethane / 2 h / 0 - 20 °C 3.1: lithium diisopropyl amide / tetrahydrofuran / 2 h / -78 °C 3.2: 7 h / -78 °C View Scheme
参考文献
SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Jiancun; ZHANG, Yingjun; ZHANG, Weihong; LIU, Bing; ZHANG, Jiquan; LIU, Jinlei; ZHANG, Lu
Patent: WO2013/71697 A1, 2013 ;
反应条件
1.1: Dess-Martin periodane / dichloromethane / 2 h / 0 - 20 °C 2.1: lithium diisopropyl amide / tetrahydrofuran / 2 h / -78 °C 2.2: 7 h / -78 °C View Scheme
参考文献
SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Jiancun; ZHANG, Yingjun; ZHANG, Weihong; LIU, Bing; ZHANG, Jiquan; LIU, Jinlei; ZHANG, Lu
Patent: WO2013/71697 A1, 2013 ;
反应条件
1.1: sodium carbonate / tetrahydrofuran; water / 0 - 20 °C 2.1: Dess-Martin periodane / dichloromethane / 2 h / 0 - 20 °C 3.1: lithium diisopropyl amide / tetrahydrofuran / 2 h / -78 °C 3.2: 7 h / -78 °C View Scheme
参考文献
SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Jiancun; ZHANG, Yingjun; ZHANG, Weihong; LIU, Bing; ZHANG, Jiquan; LIU, Jinlei; ZHANG, Lu
Patent: WO2013/71697 A1, 2013 ;
反应条件
1.1: toluene-4-sulfonic acid / toluene / |Dean-Stark; |Inert atmosphere; |Reflux 2.1: triethylamine / dichloromethane / 3 h / 0 °C / |Inert atmosphere 2.2: 1 h / |Inert atmosphere View Scheme
参考文献
Yogeeswari, Perumal; Sharma, Monika; Samala, Ganesh; Gangadhar, Matharasala; Karthick, Srirama; Mallipeddi, Saketh; Semwal, Arvind; Sriram, Dharmarajan
European Journal of Medicinal Chemistry, 2013 , vol. 66, p. 211 - 220
反应条件
hydrazine in ethanol; water
T=90°C; 2 h; Reflux;
参考文献
SUNSHINE LAKE PHARMA CO., LTD.; ZHANG, Jiancun; ZHANG, Yingjun; ZHANG, Weihong; LIU, Bing; ZHANG, Jiquan; LIU, Jinlei; ZHANG, Lu
Patent: WO2013/71697 A1, 2013 ;
Location in patent: Paragraph 00388 ;
