3-(4-氨基苯基)吡咯烷-1-羧酸叔丁酯合成路线 （共 5 条）
反应条件
palladium 10 on activated carbon; hydrogen in ethanol; water
P=22801.5 Torr;
参考文献
AFRAXIS, INC.; CAMPBELL, David; DURÓN, Sergio, G.
Patent: WO2013/43232 A2, 2013 ;
Location in patent: Paragraph 00530 ;
WO 2013/043232 A2
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: With N,N-bis(trifluoromethanesulfonyl)aniline in tetrahydrofuran
T=-78 - 20°C; 4 h;
3: p-nitrophenyl boronic acid
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; 151 ;
WO 2012/110773 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;
3: p-nitrophenyl boronic acid Further stages;
参考文献
CANCER THERAPEUTICS CRC PTY LTD; DEVLIN, Mark Graeme; STREET, Ian Philip; TONG, Warwick Bonner
Patent: WO2014/27199 A1, 2014 ;
Location in patent: Page/Page column 152-153 ;
反应条件
1.1: n-butyllithium / tetrahydrofuran; hexane / 0.83 h / -85 °C / |Inert atmosphere
1.2: |Inert atmosphere
2.1: hydrogenchloride / water; tetrahydrofuran; hexane / pH 6 - 7 / |Inert atmosphere
3.1: palladium 10 on activated carbon; hydrogen / water; ethanol / 22801.5 Torr
View Scheme
参考文献
AFRAXIS, INC.; CAMPBELL, David; DURÓN, Sergio, G.
Patent: WO2013/43232 A2, 2013 ;
WO 2013/043232 A2
反应条件
1: hydrogenchloride / water; tetrahydrofuran; hexane / pH 6 - 7 / |Inert atmosphere
2: palladium 10 on activated carbon; hydrogen / water; ethanol / 22801.5 Torr
View Scheme
参考文献
AFRAXIS, INC.; CAMPBELL, David; DURÓN, Sergio, G.
Patent: WO2013/43232 A2, 2013 ;
WO 2013/043232 A2
