3-(三氟甲磺酰基)-4-氟苯磺酰胺合成路线 （共 7 条）
反应条件
ammonia in water; isopropyl alcohol T=-78°C; 2 h;
参考文献
GENENTECH, INC.; WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH
Patent: WO2008/61208 A2, 2008 ;
Location in patent: Page/Page column 30; 31 ;
WO 2008/061208 A2
反应条件
1: With chlorosulfonic acid T=125°C; 18 h; 2: With ammonium hydroxide in isopropyl alcohol T=-65 - 0°C; 1.5 h;
参考文献
ASTRAZENECA AB
Patent: US2012/35134 A1, 2012 ;
Location in patent: Page/Page column 33 ;
反应条件
N-ethyl-N,N-diisopropylamine in 1,4-dioxane T=50°C; 4 h;
参考文献
GENENTECH, INC.; WALTER AND ELIZA HALL INSTITUTE OF MEDICAL RESEARCH
Patent: WO2008/61208 A2, 2008 ;
Location in patent: Page/Page column 38 ;
WO 2008/061208 A2
反应条件
N-ethyl-N,N-diisopropylamine 36 h;
参考文献
Porter, Jason R.; Helmers, Mark R.; Wang, Ping; Furman, Jennifer L.; Joy, Stephen T.; Arora, Paramjit S.; Ghosh, Indraneel
Chemical Communications, 2010 , vol. 46, # 42 p. 8020 - 8022
反应条件
1.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 1.5 h / 50 °C 2.1: water; lithium hydroxide hydrate / tetrahydrofuran; methanol / 3 h / 18 - 25 °C 2.2: 0 °C 3.1: N-ethyl-N,N-diisopropylamine; HATU / isobutyramide / 1 h / 18 - 25 °C View Scheme
参考文献
ASTRAZENECA AB
Patent: US2012/35134 A1, 2012 ;
反应条件
N-ethyl-N,N-diisopropylamine in dimethyl sulfoxide T=20°C; 16 h;
参考文献
Synthesis, , # 15 art. no. F04408SS, p. 2398 - 2404
反应条件
1.1: N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 1.5 h / 50 °C 2.1: water; lithium hydroxide hydrate / tetrahydrofuran; methanol / 3 h / 18 - 25 °C 2.2: 0 °C 3.1: N-ethyl-N,N-diisopropylamine; HATU / isobutyramide / 1 h / 18 - 25 °C 4.1: borane-THF / tetrahydrofuran / 18 - 25 °C 4.2: 3 h 4.3: pH ~ 10 View Scheme
