6-溴-3,4-二氢喹啉-2(1h)-硫酮合成路线 (共 5 条)
反应条件
Lawesson's reagent in toluene 0.75 h; Heating;
参考文献
Occhiato, Ernesto G.; Ferrali, Alessandro; Menchi, Gloria; Guarna, Antonio; Danza, Giovanna; Comerci, Alessandra; Mancina, Rosa; Serio, Mario; Garotta, Gianni; Cavalli, Andrea; De Vivo, Marco; Recanatini, Maurizio
Journal of Medicinal Chemistry, 2004 , vol. 47, # 14 p. 3546 - 3560
反应条件
1: 87 percent / N-bromosuccinimide / dimethylformamide / 2 h / 0 °C 2: 79 percent / Lawesson's reagent / toluene / 0.75 h / Heating View Scheme
参考文献
MERCK SHARP and DOHME CORP.; ElexoPharm GmbH; HOYT, Scott, B.; PETRILLI, Whitney Lane; LONDON, Clare; XIONG, Yusheng; TAYLOR, Jerry Andrew; ALI, Amjad; LO, Michael; HENDERSON, Timothy, J.; HU, Qingzhong; HARTMANN, Rolf; YIN, Lina; HEIM, Ralf; BEY, Emmanuel; SAXENA, Rohit; SAMANTA, Swapan Kumar; KULKARNI, Bheemashankar, A.
Patent: WO2012/148808 A1, 2012 ;
WO 2012/148808 A1
反应条件
1: dichloromethane / 2 h / 0 - 20 °C 2: AlCl3, aluminium chloride / 3 h / 120 °C 3: N-bromosuccinmide / N,N-dimethyl-formamide / 12 h / 0 - 20 °C 4: Lawesson's reagent / toluene / 3 h / 100 °C View Scheme
参考文献
MERCK SHARP and DOHME CORP.; ElexoPharm GmbH; HOYT, Scott, B.; PETRILLI, Whitney Lane; LONDON, Clare; XIONG, Yusheng; TAYLOR, Jerry Andrew; ALI, Amjad; LO, Michael; HENDERSON, Timothy, J.; HU, Qingzhong; HARTMANN, Rolf; YIN, Lina; HEIM, Ralf; BEY, Emmanuel; SAXENA, Rohit; SAMANTA, Swapan Kumar; KULKARNI, Bheemashankar, A.
Patent: WO2012/148808 A1, 2012 ;
WO 2012/148808 A1
反应条件
1: AlCl3, aluminium chloride / 3 h / 120 °C 2: N-bromosuccinmide / N,N-dimethyl-formamide / 12 h / 0 - 20 °C 3: Lawesson's reagent / toluene / 3 h / 100 °C View Scheme
参考文献
MERCK SHARP and DOHME CORP.; ElexoPharm GmbH; HOYT, Scott, B.; PETRILLI, Whitney Lane; LONDON, Clare; XIONG, Yusheng; TAYLOR, Jerry Andrew; ALI, Amjad; LO, Michael; HENDERSON, Timothy, J.; HU, Qingzhong; HARTMANN, Rolf; YIN, Lina; HEIM, Ralf; BEY, Emmanuel; SAXENA, Rohit; SAMANTA, Swapan Kumar; KULKARNI, Bheemashankar, A.
Patent: WO2012/148808 A1, 2012 ;
WO 2012/148808 A1
反应条件
1.1: 22 percent / K2CO3; 18-crown-6 / tetrahydrofuran / 3 h / 20 °C
2.1: toluene / 0.25 h / Heating
2.2: 42 percent / DBU / toluene / 0.33 h / Heating
View Scheme
参考文献
Occhiato, Ernesto G.; Ferrali, Alessandro; Menchi, Gloria; Guarna, Antonio; Danza, Giovanna; Comerci, Alessandra; Mancina, Rosa; Serio, Mario; Garotta, Gianni; Cavalli, Andrea; De Vivo, Marco; Recanatini, Maurizio
Journal of Medicinal Chemistry, 2004 , vol. 47, # 14 p. 3546 - 3560