2-(2-甲基-5-溴苄基)-5-(4-氟苯)噻吩合成路线 (共 6 条)
反应条件
triethylsilane; boron trifluoride diethyl etherate in dichloromethane T=0 - 20°C; Inert atmosphere;
参考文献
Nomura, Sumihiro; Sakamaki, Shigeki; Hongu, Mitsuya; Kawanishi, Eiji; Koga, Yuichi; Sakamoto, Toshiaki; Yamamoto, Yasuo; Ueta, Kiichiro; Kimata, Hirotaka; Nakayama, Keiko; Tsuda-Tsukimoto, Minoru
Journal of Medicinal Chemistry, 2010 , vol. 53, # 17 p. 6355 - 6360
反应条件
1.1: potassium carbonate / tri-cyclo-hexyl-phosphine; tris-(dibenzylideneacetone)dipalladium(0) / ethanol; water / 90 °C / Inert atmosphere 2.1: AlCl3, aluminium chloride / dichloromethane / 0 - 20 °C 2.2: cooling with ice 3.1: boron trifluoride diethyl etherate; triethylsilane / dichloromethane; acetonitrile / 3 h / 0 - 20 °C View Scheme
参考文献
WO2012/160218 A1, ;
WO 2012/160218 A1
反应条件
1.1: oxalyl dichloride / N,N-dimethyl-formamide / dichloromethane / 6 h / 20 °C 2.1: AlCl3, aluminium chloride / dichloromethane / 0 - 20 °C 2.2: cooling with ice 3.1: boron trifluoride diethyl etherate; triethylsilane / dichloromethane; acetonitrile / 3 h / 0 - 20 °C View Scheme
参考文献
WO2012/160218 A1, ;
WO 2012/160218 A1
反应条件
1.1: AlCl3, aluminium chloride / dichloromethane / 0 - 20 °C 1.2: cooling with ice 2.1: boron trifluoride diethyl etherate; triethylsilane / dichloromethane; acetonitrile / 3 h / 0 - 20 °C View Scheme
参考文献
WO2012/160218 A1, ;
WO 2012/160218 A1
反应条件
1.1: AlCl3, aluminium chloride / dichloromethane / 0 - 20 °C 1.2: cooling with ice 2.1: boron trifluoride diethyl etherate; triethylsilane / dichloromethane; acetonitrile / 3 h / 0 - 20 °C View Scheme
参考文献
WO2012/160218 A1, ;
WO 2012/160218 A1
反应条件
sodium iodide; N-methyl-2-(methylamino)ethylamine; copper(l) iodide in diethylene glycol dimethyl ether; toluene T=110°C;
参考文献
Fillers, Walter Ferdinand Maria; Broeckx, Rudy Laurent Maria; Nieste, Patrick Hubert J.; Hatsuda, Masanori; Yoshinaga, Masahiko; Yada, Mitsuhiro
Patent: US2010/99883 A1, 2010 ;
Location in patent: Page/Page column 43 ;
US 20100099883 A1