7-硝基-1,2,3,4-四氢异喹啉合成路线 （共 24 条）
反应条件
1: 1.7 g / 88 percent formic acid / H2O / 2 h / 80 °C
2: 99 percent / H2 / 10 percent Pd/C / methanol
View Scheme
参考文献
GLAXOSMITHKLINE LLC; KALLANDER, Lara, S.; LAWHORN, Brian, Griffin; PHILIP, Joanne; ZHAO, Yongdong
Patent: WO2011/88027 A1, 2011 ;
反应条件
sodium tris(acetoxy)borohydride in acetic acid; 1,2-dichloro-ethane
T=25°C; Reduction; alkylation; 72 h;
参考文献
Chan, Wai N.; Hadley, Michael S.; Harling, John D.; Herdon, Hugh J.; Orlek, Barry S.; Riley, Graham J.; Stead, Rachel E. A.; Stean, Tania O.; Thompson, Mervyn; Upton, Neil; Ward, Robert W.
Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 8 p. 2085 - 2094
反应条件
1.1: 94 percent / Et3N / CH2Cl2 / 1 h / Heating
2.1: FeCl3*6H2O; activated carbon / methanol / 0.33 h / Heating
2.2: 85 percent / NH2NH2*H2O / methanol / 4 h / Heating
View Scheme
参考文献
Zhu, Zhengxiang; Furr, John; Buolamwini, John K.
Journal of Medicinal Chemistry, 2003 , vol. 46, # 5 p. 831 - 837
反应条件
1.1: 94 percent / Et3N / CH2Cl2 / 1 h / Heating
2.1: FeCl3*6H2O; activated carbon / methanol / 0.33 h / Heating
2.2: 85 percent / NH2NH2*H2O / methanol / 4 h / Heating
3.1: 94 percent / TFA / CH2Cl2 / 0.25 h / Heating
4.1: H2SO4; KNO3 / 0 °C
4.2: 0.5 g / aq. HCl / methanol / 0.83 h / Heating
5.1: aq. NaNO2; aq. HCl / 2 h / 0 °C
5.2: 86 percent / aq. H3PO2 / 10 h / 40 °C
6.1: aq. HCl / methanol / 10 h / Heating
View Scheme
参考文献
Zhu, Zhengxiang; Furr, John; Buolamwini, John K.
Journal of Medicinal Chemistry, 2003 , vol. 46, # 5 p. 831 - 837
