1-苄基-5-(4,4,5,5-四甲基-1,3,2-二噁硼烷-2-基)-1,2,3,6-四氢吡啶合成路线 (共 4 条)
反应条件
potassium acetate; 1,1'-bis-(diphenylphosphino)ferrocene; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride in 1,4-dioxane T=80°C; 4 h;
参考文献
ELI LILLY AND COMPANY
Patent: WO2004/26305 A1, 2004 ;
Location in patent: Page/Page column 179-180 ;
WO 2004/026305 A1
反应条件
1,1'-bis-(diphenylphosphino)ferrocene; potassium acetate; dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct in 1,4-dioxane T=80°C; 3 h; Inert atmosphere;
参考文献
ADVINUS THERAPEUTICS LIMITED; BARAWKAR, Dinesh; BENDE, Tanushree; ZAHLER, Robert; BANDYOPADHYAY, Anish; SARANGTHEM, Robindro Singh; DOSHI, Jignesh; WAMAN, Yogesh; JADHAV, Rushikesh; SINGH, Umesh Prasad
Patent: WO2012/127506 A1, 2012 ;
Location in patent: Page/Page column 72 ;
WO 2012/127506 A1
反应条件
1.1: N-ethyl-N,N-diisopropylamine; n-butyllithium / tetrahydrofuran / 1 h / -78 °C 1.2: -78 - 20 °C 2.1: 1,1'-bis-(diphenylphosphino)ferrocene; potassium acetate / dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct / 1,4-dioxane / 3 h / 80 °C / Inert atmosphere View Scheme
参考文献
ADVINUS THERAPEUTICS LIMITED; BARAWKAR, Dinesh; BENDE, Tanushree; ZAHLER, Robert; BANDYOPADHYAY, Anish; SARANGTHEM, Robindro Singh; DOSHI, Jignesh; WAMAN, Yogesh; JADHAV, Rushikesh; SINGH, Umesh Prasad
Patent: WO2012/127506 A1, 2012 ;
WO 2012/127506 A1
反应条件
1.1: sodium carbonate / water 2.1: N-ethyl-N,N-diisopropylamine; n-butyllithium / tetrahydrofuran / 1 h / -78 °C 2.2: -78 - 20 °C 3.1: 1,1'-bis-(diphenylphosphino)ferrocene; potassium acetate / dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II) dichloromethane adduct / 1,4-dioxane / 3 h / 80 °C / Inert atmosphere View Scheme
参考文献
ADVINUS THERAPEUTICS LIMITED; BARAWKAR, Dinesh; BENDE, Tanushree; ZAHLER, Robert; BANDYOPADHYAY, Anish; SARANGTHEM, Robindro Singh; DOSHI, Jignesh; WAMAN, Yogesh; JADHAV, Rushikesh; SINGH, Umesh Prasad
Patent: WO2012/127506 A1, 2012 ;
WO 2012/127506 A1