5-羟基异吲哚啉-2-羧酸叔丁酯合成路线 (共 5 条)
反应条件
1: 5-hydroxy-isoindoline hydrobromide With sodium hydrogencarbonate in water T=3°C; 0.25 h; 2: di-tert-butyl dicarbonate in tetrahydrofuran; water T=3 - 20°C; 4 h;
参考文献
PFIZER PRODUCTS INC.
Patent: WO2008/20306 A2, 2008 ;
Location in patent: Page/Page column 22; 24 ;
反应条件
1: 4-hydroxyphthalimide With borane-THF in tetrahydrofuran T=-5 - 80°C; 19 h; 2: With hydrogenchloride in methanol; water T=0 - 80°C; 3 h; 3: di-tert-butyl dicarbonate With triethylamine in methanol; water T=22°C; 0.5 h;
参考文献
Merck Patent Gesellschaft Mit Beschrankter Haftung
Patent: US2010/311745 A1, 2010 ;
Location in patent: Page/Page column 18 ;
反应条件
triethylamine in dichloromethane T=20°C; 16 h;
参考文献
Austin, Nigel E; Avenell, Kim Y; Boyfield, Izzy; Branch, Clive L; Hadley, Michael S; Jeffrey, Phillip; Johnson, Christopher N; Macdonald, Gregor J; Nash, David J; Riley, Graham J; Smith, Alexander B; Stemp, Geoffrey; Thewlis, Kevin M; Vong, Antonio K.K; Wood, Martyn D
Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 5 p. 685 - 688
反应条件
1: 80 percent / aq. HBr / 2 h / 100 °C 2: 40 percent / Et3N / CH2Cl2 / 16 h / 20 °C View Scheme
参考文献
Austin, Nigel E; Avenell, Kim Y; Boyfield, Izzy; Branch, Clive L; Hadley, Michael S; Jeffrey, Phillip; Johnson, Christopher N; Macdonald, Gregor J; Nash, David J; Riley, Graham J; Smith, Alexander B; Stemp, Geoffrey; Thewlis, Kevin M; Vong, Antonio K.K; Wood, Martyn D
Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 5 p. 685 - 688
反应条件
1: 70 percent / Et3N / CH2Cl2 / 6 h / -20 - 20 °C 2: 90 percent / Pd(PPh3)4 / dimethylformamide / 4 h / 100 °C View Scheme
参考文献
Austin, Nigel E; Avenell, Kim Y; Boyfield, Izzy; Branch, Clive L; Hadley, Michael S; Jeffrey, Phillip; Johnson, Christopher N; Macdonald, Gregor J; Nash, David J; Riley, Graham J; Smith, Alexander B; Stemp, Geoffrey; Thewlis, Kevin M; Vong, Antonio K.K; Wood, Martyn D
Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 5 p. 685 - 688