N,N-二甲基-4-(4,4,5,5-四甲基-1,3,2-二噁硼烷-2-基)-1H-吡唑-1-乙胺合成路线 (共 6 条)
反应条件
caesium carbonate in acetonitrile
5 h; Reflux;
参考文献
GLAXOSMITHKLINE LLC; DEMONT, Emmanuel, Hubert; GARTON, Neil, Stuart; GOSMINI, Romain, Luc, Marie; HAYHOW, Thomas, George, Christopher; SEAL, Jonathan; WILSON, David, Matthew; WOODROW, Michael, David
Patent: WO2011/54841 A1, 2011 ;
Location in patent: Page/Page column 105 ;
反应条件
1: in tetrahydrofuran
T=20°C; 48 h;
2: With potassium iodide in tetrahydrofuran
T=75°C; 48 h;
参考文献
ASTRAZENECA AB; NPS PHARMACEUTICALS, INC.
Patent: WO2006/20879 A1, 2006 ;
Location in patent: Page/Page column 111 ;
WO 2006/020879 A1
反应条件
potassium carbonate in N,N-dimethyl-formamide
T=190°C; 1 h; Microwave irradiation;
参考文献
Dinsmore, Christopher J.; Gabarda Ortega, Ana Esther; Guerin, David J.; Jewell, James P.; Katz, Jason D.; Lim, Jongwon; Machacek, Michelle R.; Otte, Ryan D.; Young, Jonathan R.
Patent: US2006/293358 A1, 2006 ;
Location in patent: Page/Page column 48 ;
US 20060293358 A1
反应条件
(1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; potassium acetate in 1,4-dioxane
T=100°C; 12 h; Inert atmosphereSealed tube;
参考文献
ORION CORPORATION; LINNANEN, Tero; WOHLFAHRT, Gerd; NANDURI, Srinivas; UJJINAMATADA, Ravi; RAJAGOPALAN, Srinivasan; MUKHERJEE, Subhendu
Patent: WO2013/53983 A1, 2013 ;
Location in patent: Page/Page column 29 ;
反应条件
1: 2-(1H-Pyrazole-4-yl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane With caesium carbonate in acetonitrile
T=20°C; 0.25 h;
2: 2-dimethylamino-1-chloro-ethane hydrochloride in acetonitrile
T=20°C; 48 h;
参考文献
MERCK PATENT GESELLSCHAFT
Patent: US2011/218198 A1, 2011 ;
Location in patent: Page/Page column 15-16 ;
反应条件
1: caesium carbonate / acetonitrile / 5 h / 75 °C
2: sodium iodide / N,N-dimethyl-formamide; tetrahydrofuran / 80 °C
View Scheme
参考文献
INCYTE CORPORATION; Li, Yun-Long; Yao, Wenqing; Combs, Andrew P.; Yue, Eddy W.; Mei, Song; Zhu, Wenyu; Glenn, Joseph; Maduskuie, JR., Thomas P.; Sparks, Richard B.; Douty, Brent
Patent: US2013/59835 A1, 2013 ;