4-(乙酰基硫代)-1-哌啶羧酸苄酯合成路线 （共 11 条）
反应条件
potassium thiosulphate in DMF (N,N-dimethyl-formamide) T=20 - 60°C; 19 h;
参考文献
Sumitomo Pharmaceuticals Company, Limited
Patent: EP1403255 A1, 2004 ;
Location in patent: Page 90 ;
EP 1403255 A1
反应条件
1: 4-Hydroxy-piperidine-1-carboxylic acid benzyl ester With methanesulfonyl chloride; triethylamine in dichloromethane T=0 - 20°C; 48 h; 2: thiolacetic acid potassium salt in dichloromethane T=90°C; 3 h;
参考文献
ASTRAZENECA AB
Patent: WO2005/7629 A1, 2005 ;
Location in patent: Page 45-46 ;
WO 2005/007629 A1
反应条件
in dimethyl sulfoxide 21.5 h;
参考文献
SCHERING CORPORATION
Patent: WO2003/103669 A1, 2003 ;
Location in patent: Page 44-45 ;
WO 03/103669 A1
反应条件
potassium carbonate in N,N-dimethyl-formamide T=10 - 80°C;
参考文献
Zhersh, Sergey; Buryanov, Volodymyr V.; Karpenko, Oleksandr V.; Grygorenko, Oleksandr O.; Tolmachev, Andrey A.
Synthesis, 2011 , # 22 art. no. Z72611SS, p. 3669 - 3674
反应条件
1: triethylamine 2: triethylamine / dichloromethane / 0 °C 3: potassium carbonate / N,N-dimethyl-formamide / 10 - 80 °C View Scheme
参考文献
Zhersh, Sergey; Buryanov, Volodymyr V.; Karpenko, Oleksandr V.; Grygorenko, Oleksandr O.; Tolmachev, Andrey A.
Synthesis, 2011 , # 22 art. no. Z72611SS, p. 3669 - 3674
反应条件
1: triethylamine / dichloromethane / 0 °C 2: potassium carbonate / N,N-dimethyl-formamide / 10 - 80 °C View Scheme
参考文献
Zhersh, Sergey; Buryanov, Volodymyr V.; Karpenko, Oleksandr V.; Grygorenko, Oleksandr O.; Tolmachev, Andrey A.
Synthesis, 2011 , # 22 art. no. Z72611SS, p. 3669 - 3674
反应条件
1: triethylamine 2: triethylamine / dichloromethane / 0 °C 3: potassium carbonate / N,N-dimethyl-formamide / 10 - 80 °C View Scheme
参考文献
Zhersh, Sergey; Buryanov, Volodymyr V.; Karpenko, Oleksandr V.; Grygorenko, Oleksandr O.; Tolmachev, Andrey A.
Synthesis, 2011 , # 22 art. no. Z72611SS, p. 3669 - 3674
反应条件
triphenylphosphine; diethylazodicarboxylate 1.) THF, -78 deg C, 7 min, 2.) THF, a) -78 deg C, 1 h, b) RT, 20 h; Yield given. Multistep reaction;
参考文献
Rosenberg; Spina; Condon; Polakowski; Yao; Kovar; Stein; Cohen; Barlow; Klinghofer; Egan; Tricarico; Perun; Baker; Kleinert
Journal of Medicinal Chemistry, 1993 , vol. 36, # 4 p. 460 - 467
反应条件
chlorine in dichloromethane; water T=0°C; 4 h;
参考文献
EP1403255 A1, ;
Page 90 ;
EP 1403255 A1
反应条件
in water T=0°C; 0.5 h;
参考文献
WO2003/103669 A1, ;
Page 44-45 ;
WO 03/103669 A1
