5-溴-2-三氟甲基吡啶合成路线 (共 22 条)
反应条件
1: (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; N-ethyl-N,N-diisopropylamine / 12 h / 100 °C / 2585.81 Torr
2: tetrahydrofuran / 2 h / -10 °C
3: toluene-4-sulfonic acid / toluene / 6 h / Reflux
View Scheme
参考文献
Butcher, Kenneth J.; Denton, Steven M.; Field, Stuart E.; Gillmore, Adam T.; Harbottle, Gareth W.; Howard, Roger M.; Laity, Daniel A.; Ngono, Christian J.; Pibworth, Benjamin A.
Organic Process Research and Development, 2011 , vol. 15, # 5 p. 1192 - 1200
反应条件
1: N-[(1,1-dimethylethoxy)carbonyl]-3-iodo-L-alanine methyl ester With chloro-trimethyl-silane; ethylene dibromide; zinc in N,N-dimethyl-formamide
T=20°C;
2: 5-bromo-2-(trifluoromethyl)pyridine With bis-triphenylphosphine-palladium(II) chloride in N,N-dimethyl-formamide
T=25°C;
参考文献
AMGEN INC.; ZENG, Qingping; YUAN, Chester Chenguang; YAO, Guomin; WANG, Xianghong; TADESSE, Seifu; ST. JEAN, JR., David J.; REICHELT, Andreas; LIU, Qingyian; HONG, Fang-Tsao; HAN, Nianhe; FOTSCH, Christopher H.; DAVIS, Carl D.; BOURBEAU, Matthew P.; ASHTON, Kate S.; ALLEN, John G.
Patent: WO2010/83246 A1, 2010 ;
Location in patent: Page/Page column 57 ;