3-(三氟甲基磺酰氧基)-2H-吡咯-1(5h)-羧酸叔丁酯合成路线 (共 5 条)
反应条件
potassium acetate; 1,1'-bis-(diphenylphosphino)ferrocene; dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct in 1,4-dioxane T=80°C; Inert atmosphere;
参考文献
US2010/204265 A1, ;
Page/Page column 91; 92 ;
反应条件
1: 3-Oxo-pyrrolidine-1-carboxylic acid tert-butyl ester With lithium hexamethyldisilazane in tetrahydrofuran
T=-78°C; 1 h;
2: N-(5-chloropyridin-2-yl)-1,1,1-trifluoro-N-[(trifluoromethyl)sulfonyl]methanesulfonamide in tetrahydrofuran
T=-78 - 20°C; 3.5 h;
参考文献
Purandare, Ashok Vinayak; Wan, Honghe; Huynh, Tram N.
Patent: US2006/235037 A1, 2006 ;
Location in patent: Page/Page column 60 ;
US 20060235037 A1
反应条件
1: 3-Oxo-pyrrolidine-1-carboxylic acid tert-butyl ester With sodium hexamethyldisilazane in tetrahydrofuran
T=-75°C; 0.5 h;
2: N,N-bis(trifluoromethanesulfonyl)aniline in tetrahydrofuran
T=-75 - 0°C;
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 151 ;
WO 2010/005783 A1
反应条件
1: 3-Oxo-pyrrolidine-1-carboxylic acid tert-butyl ester With sodium hexamethyldisilazane in tetrahydrofuran
T=-78°C; 0.25 h;
2: N,N-bis(trifluoromethanesulfonyl)aniline in tetrahydrofuran
T=-78 - 20°C; 4 h;
参考文献
CANCER THERAPEUTICS CRC PTY LIMITED; HOLMES, Ian, Peter; BERGMAN, Ylva; LUNNISS, Gillian Elizabeth; NIKAC, Marica; CHOI, Neil; HEMLEY, Catherine Fae; WALKER, Scott Raymond; FOITZIK, Richard Charles; GANAME, Danny; LESSENE, Romina
Patent: WO2012/110773 A1, 2012 ;
Location in patent: Page/Page column 149; 150 ;
WO 2012/110773 A1
反应条件
n-butyllithium; diisopropylamine in tetrahydrofuran; hexane
T=-78 - 20°C; 14.25 h;
参考文献
SANOFI-AVENTIS
Patent: US2009/176775 A1, 2009 ;
Location in patent: Page/Page column 33-34 ;