3,6-二氢-4-[[(三氟甲基)磺酰]氧基]-1(2H)-吡啶甲酸叔丁酯合成路线 （共 52 条）
反应条件
1: tert-butyl 4-oxo-piperidine-1-carboxylate With n-butyllithium; diisopropylamine in tetrahydrofuran T=-78°C; 1.25 h; 2: N,N-bis(trifluoromethanesulfonyl)aniline in tetrahydrofuran T=-78 - 20°C;
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED
Patent: WO2007/60409 A1, 2007 ;
Location in patent: Page/Page column 87-88 ;
WO 2007/060409 A1
反应条件
1: tert-butyl 4-oxo-piperidine-1-carboxylate With lithium hexamethyldisilazane in tetrahydrofuran T=-78°C; 0.333333 h; 2: N-phenyl-1,1,1-trifluoromethanesulfonamide in tetrahydrofuran T=-78 - 0°C; 3 h;
参考文献
INCYTE CORPORATION
Patent: WO2005/37826 A1, 2005 ;
Location in patent: Page/Page column 90 ;
WO 2005/037826 A1
反应条件
1: tert-butyl 4-oxo-piperidine-1-carboxylate With lithium hexamethyldisilazane in tetrahydrofuran T=-75°C; 0.5 h; 2: N,N-bis(trifluoromethanesulfonyl)aniline in tetrahydrofuran T=-75 - 0°C; 3: With water in tetrahydrofuran; ethyl acetate 0.166667 h; Cooling;
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG; BENTZIEN, Joerg, Martin; BOYER, Stephen, James; BURKE, Jennifer; ELDRUP, Anne, Bettina; GUO, Xin; HUBER, John, David; KIRRANE, Thomas, Martin; SOLEYMANZADEH, Fariba; SWINAMER, Alan, David
Patent: WO2010/5783 A1, 2010 ;
Location in patent: Page/Page column 115 ;
WO 2010/005783 A1
反应条件
1: tert-butyl 4-oxo-piperidine-1-carboxylate With lithium diisopropyl amide in tetrahydrofuran; Petroleum ether T=-78°C; 0.333333 h; 2: N-phenyl-1,1,1-trifluoromethanesulfonamide in tetrahydrofuran; Petroleum ether T=0°C; 3.5 h; Further stages.;
参考文献
Bursavich; West; Rich
Organic letters, 2001 , vol. 3, # 15 p. 2317 - 2320
反应条件
lithium hexamethyldisilazane in tetrahydrofuran T=-78 - 20°C; 6 h; Inert atmosphere;
参考文献
ABBOTT LABORATORIES; ABBOTT LABORATORIES TRADING (SHANGHAI) COMPANY, LTD.; WANG, Xueqing; MEYER, Michael; YAO, Betty; GUO, Tao; WEI, Guo Ping,Robert; WANG, Lijuan, Jane
Patent: WO2013/10453 A1, 2013 ;
Location in patent: Page/Page column 101 ;
反应条件
1: tert-butyl 4-oxo-piperidine-1-carboxylate With lithium diisopropyl amide in tetrahydrofuran; hexane T=-78°C; 2 h; 2: N-(5-chloropyridin-2-yl)-1,1,1-trifluoro-N-[(trifluoromethyl)sulfonyl]methanesulfonamide in tetrahydrofuran; hexane T=-78°C; 12 h;
参考文献
Hanessian, Stephen; Yang, Gaoqiang; Rondeau, Jean-Michel; Neumann, Ulf; Betschart, Claudia; Tintelnot-Blomley, Marina
Journal of Medicinal Chemistry, 2006 , vol. 49, # 15 p. 4544 - 4567
反应条件
water; triethylamine in dichloromethane T=-30°C; 1 h;
参考文献
WO2004/5256 A2, ;
Page 28 ;
WO 2004/005256 A2
反应条件
lithium hexamethyldisilazane in tetrahydrofuran; ethyl acetate
参考文献
US5665719 A1, ;
US 5665719 A
反应条件
1: tert-butyl 4-oxo-piperidine-1-carboxylate With lithium diisopropyl amide in tetrahydrofuran 0.5 h; 2: Tf2NPh in tetrahydrofuran T=20°C;
参考文献
WO2004/58727 A1, ;
Page 52 ;
反应条件
1: tert-butyl 4-oxo-piperidine-1-carboxylate With n-butyllithium; diisopropylamine in tetrahydrofuran; hexane T=-78°C; 2 h; 2: PhN(OTf)2 in tetrahydrofuran; hexane T=-78°C; Cooling;
参考文献
Okitsu, Takashi; Iwatsuka, Kinya; Wada, Akimori
Chemical Communications, 2008 , # 47 p. 6330 - 6332
