5-[4’-(溴甲基)-[1,1’-联苯]-2-基]-2-(三苯基甲基)-2H-四氮唑合成路线 （共 23 条）
反应条件
1.1: 2,2,6,6-tetramethylpiperidinyl-lithium; n-butyllithium / tetrahydrofuran; hexane / 0.08 h / -78 - -10 °C / |Inert atmosphere 1.2: 5 h / -78 - 20 °C / |Inert atmosphere 2.1: toluene / 20 °C 3.1: potassium carbonate; tetrakis(triphenylphosphine) palladium(0) / toluene; ethanol / 4 h / 100 °C / |Inert atmosphere 4.1: trimethylsilylazide; trifluoroacetic acid / 36 h / 120 °C / |Sealed tube 5.1: triethylamine / dichloromethane / 1 h / 20 °C 6.1: dibenzoyl peroxide; N-bromosuccinmide / tetrachloromethane / 8 h / |Reflux View Scheme
参考文献
European Journal of Medicinal Chemistry, , vol. 55, p. 358 - 374,17
European Journal of Medicinal Chemistry, , vol. 55, p. 358 - 374
反应条件
1: potassium carbonate; tetrakis(triphenylphosphine) palladium(0) / toluene; ethanol / 4 h / 100 °C / |Inert atmosphere 2: trimethylsilylazide; trifluoroacetic acid / 36 h / 120 °C / |Sealed tube 3: triethylamine / dichloromethane / 1 h / 20 °C 4: dibenzoyl peroxide; N-bromosuccinmide / tetrachloromethane / 8 h / |Reflux View Scheme
参考文献
European Journal of Medicinal Chemistry, , vol. 55, p. 358 - 374,17
European Journal of Medicinal Chemistry, , vol. 55, p. 358 - 374
反应条件
1: triethylamine / dichloromethane / 1 h / 20 °C 2: N-bromosuccinmide; dibenzoyl peroxide / tetrachloromethane / 8 h / Reflux View Scheme
参考文献
Journal of Computer-Aided Molecular Design, , vol. 24, # 9 p. 749 - 758
反应条件
1: 1.) t-BuOK / 1.) DMA, 0 deg C, 10 min, 2.) DMA, RT, 1 h 2: LiOH*H2O / dioxane; H2O / 20 h / Ambient temperature 3: 88 percent / K2CO3 / N,N-dimethyl-acetamide / 4 h / 20 - 50 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 39, # 1 p. 323 - 338
反应条件
1: tetrahydrofuran / 2 h / Ambient temperature 2: Et3N / tetrahydrofuran / 2 h 3: 88percent aq. HCOOH / CH2Cl2 / 2 h / Ambient temperature 4: aq. NaOH / ethanol / 24 h / Ambient temperature View Scheme
参考文献
De, B.; Winn, M.; Zydowsky, T. M.; Kerkman, D. J.; DeBernardis, J. F.; et al.
Journal of Medicinal Chemistry, 1992 , vol. 35, # 20 p. 3714 - 3717
反应条件
1: With potassium carbonate in N,N-dimethyl-formamide T=20 - 22°C; 3 h; 2: With sodium tetrahydroborate in water; N,N-dimethyl-formamide T=48 - 52°C; 3.08333 h;
参考文献
MEDICHEM, S.A.
Patent: WO2007/20533 A2, 2007 ;
Location in patent: Page/Page column 11-12 ;
反应条件
potassium carbonate in N,N-dimethyl-formamide T=20°C; 10 h;
参考文献
Sieron, Leslaw; Nagaraj; Prabhuswamy; Yathirajan; Nagaraja; Narasegowda; Gaonkar
Acta Crystallographica Section C: Crystal Structure Communications, 2004 , vol. 60, # 11 p. o821-o823
反应条件
1: 49 percent / potassium carbonate / dimethylformamide / 24 h / 25 °C 2: sodium borohydride / CH2Cl2 / 24 h / 25 °C View Scheme
参考文献
Carini, David J.; Duncia, John V.; Aldrich, Paul E.; Chiu, Andrew T.; Johnson, Alexander L.; et al.
Journal of Medicinal Chemistry, 1991 , vol. 34, # 8 p. 2525 - 2547
反应条件
potassium carbonate in N,N-dimethyl-formamide Ambient temperaturevarious ratios of reagents; Product distribution;
参考文献
Pierce, Michael E.; Carini, David J.; Huhn, George F.; Wells, Gregory J.; Arnett, John F.
Journal of Organic Chemistry, 1993 , vol. 58, # 17 p. 4642 - 4645
反应条件
1: 1.) t-BuOK / 1.) DMA, 0 deg C, 10 min, 2.) DMA, RT, 1 h 2: LiOH*H2O / dioxane; H2O / 20 h / Ambient temperature 3: 88 percent / K2CO3 / N,N-dimethyl-acetamide / 4 h / 20 - 50 °C 4: 81 percent / 25percent aq. AcOH / 2.5 h / 80 °C View Scheme
参考文献
Yanagisawa, Hiroaki; Amemiya, Yoshiya; Kanazaki, Takuro; Shimoji, Yasuo; Fujimoto, Koichi; Kitahara, Yoshiko; Sada, Toshio; Mizuno, Makoto; Ikeda, Masahiro; Miyamoto, Shuichi; Furukawa, Youji; Koike, Hiroyuki
Journal of Medicinal Chemistry, 1996 , vol. 39, # 1 p. 323 - 338
