3,3-二甲基-1-苯基甲基-4-哌啶酮合成路线 （共 13 条）
反应条件
1: With dimethyl sulfoxide; trifluoroacetic anhydride in dichloromethane T=-78°C; 0.5 h; 2: (rac)-1-Benzyl-3,3-dimethyl-piperidin-4-ol in dichloromethane T=-78°C; 1 h; 3: With triethylamine in dichloromethane T=0°C; 2 h;
参考文献
ELI LILLY AND COMPANY
Patent: EP1204660 B1, 2004 ;
Location in patent: Page 15 ;
反应条件
sodium t-butanolate in tetrahydrofuran T=0 - 20°C;
参考文献
Millennium Pharmaceuticals, Inc.
Patent: US2002/169155 A1, 2002 ;
US 20020169155 A1
反应条件
1: formaldehyd; benzylamine in ethanol T=10°C; 2: 3-methyl-butan-2-one With hydrogenchloride in ethanol Heating / reflux; 3: N-ethyl-N,N-diisopropylamine With potassium hydroxide; formaldehyd more than 3 stages;
参考文献
He, John Xiaoqiang; Honigschmidt, Nicholas Allan; Kohn, Todd Jonathan; Rocco, Vincent Patrick; Spinazze, Patrick Gianpietro; Takeuchi, Kumiko
Patent: US2003/225281 A1, 2003 ;
Location in patent: Page 15 ;
反应条件
1: With hydrogenchloride in ethanol; water Cooling with iceReflux; 2: With N-ethyl-N,N-diisopropylamine in ethanol; water T=20°C; Reflux;
参考文献
Takeda Pharmaceutical Company Limited
Patent: EP2216023 A1, 2010 ;
Location in patent: Page/Page column 115-116 ;
EP 2216023 A1
反应条件
formaldehyd; N-ethyl-N,N-diisopropylamine in ethanol; dichloromethane; water
参考文献
Eli Lilly and Company
Patent: US6538136 B1, 2003 ;
反应条件
hydrogenchloride; formaldehyd; N-ethyl-N,N-diisopropylamine; benzylamine in ethanol 6 h; Heating / reflux;
参考文献
He, John Xiaoqiang; Honigschmidt, Nicholas Allan; Kohn, Todd Jonathan; Rocco, Vincent Patrick; Spinazze, Patrick Gianpietro; Takeuchi, Kumiko
Patent: US2003/232833 A1, 2003 ;
Location in patent: Page 16 ;
反应条件
sodium hydride in tetrahydrofuran T=20 - 60°C; 5.08333 h;
参考文献
WARNER-LAMBERT COMPANY LLC
Patent: WO2005/26145 A2, 2005 ;
Location in patent: Page/Page column 102; 103 ;
反应条件
1: 1-Phenylmethyl-piperidin-4-one With sodium hydride in tetrahydrofuran T=-5°C; 1 h; 2: methyl iodide in tetrahydrofuran T=0 - 20°C; 4 h; 3: With ammonium chloride in tetrahydrofuran; water
参考文献
SCHERING CORPORATION
Patent: WO2008/130584 A1, 2008 ;
Location in patent: Page/Page column 161 ;
WO 2008/130584 A1
反应条件
hydrogenchloride; potassium hydroxide; formaldehyd; triethylamine in ethanol; water
参考文献
Eli Lilly and Company
Patent: US6538136 B1, 2003 ;
反应条件
hydrogen; palladium 10 on activated carbon in methanol T=20°C; P=3345.86 Torr; 16 h;
参考文献
ELI LILLY AND COMPANY
Patent: EP1204660 B1, 2004 ;
Location in patent: Page 18 ;
