5-羟基吲哚-2-甲酸乙酯合成路线 （共 8 条）
反应条件
hydrogen; palladium on activated charcoal in ethanol
参考文献
SmithKline Beecham Corporation
Patent: US6469046 B1, 2002 ;
US 6469046 B1
反应条件
boron tribromide in dichloromethane
参考文献
Dawson, Marcia J.; Fontana, Joseph A.; Zhang, Xiao-kun; Leid, Mark; Jong, Ling; Hobbs, Peter D.
Patent: US2003/176506 A1, 2003 ;
反应条件
thionyl chloride T=80°C; 0.5 h; Microwave irradiation;
参考文献
Frecentese, Francesco; Fiorino, Ferdinando; Perissutti, Elisa; Severino, Beatrice; Magli, Elisa; Esposito, Antonella; De Angelis, Francesca; Massarelli, Paola; Nencini, Cristina; Viti, Barbara; Santagada, Vincenzo; Caliendo, Giuseppe
European Journal of Medicinal Chemistry, 2010 , vol. 45, # 2 p. 752 - 759
反应条件
4-(N,N-dimethlyamino)pyridine in acetic anhydride; ethyl acetate
参考文献
AstraZeneca AB
Patent: US6984657 B1, 2006 ;
US 6984657 B1
反应条件
4-(N,N-dimethlyamino)pyridine T=80°C; 4 h;
参考文献
AstraZeneca AB
Patent: US6737435 B1, 2004 ;
Location in patent: Page/Page column 19 ;
US 6737435 B1
反应条件
1: 94 percent / Fremy's salt, KH2PO4 / acetonitrile; H2O / 0.5 h / 20 °C 2: 47 percent / Et3N / tetrahydrofuran / 1 h / 20 °C 3: 1.) N-chlorosuccinimide, triethylamine; 2.) DDQ, Et3N / 1.) methylene chloride, 20 deg C, 30 min; 2.) methylene chloride, 20 deg C, 90 min 4: 85 percent / trifluoroacetic acid / 1 h / 20 °C 5: 82 percent / chlorobenzene / 4 h / 131 °C 6: LiOH View Scheme
参考文献
Journal of the American Chemical Society, , vol. 107, # 19 p. 5555 - 5556
反应条件
1: 94 percent / Fremy's salt, KH2PO4 / acetonitrile; H2O / 0.5 h / 20 °C
2: 47 percent / Et3N / tetrahydrofuran / 1 h / 20 °C
3: 1.) N-chlorosuccinimide, triethylamine; 2.) DDQ, Et3N / 1.) methylene chloride, 20 deg C, 30 min; 2.) methylene chloride, 20 deg C, 90 min
4: 85 percent / trifluoroacetic acid / 1 h / 20 °C
5: 82 percent / chlorobenzene / 4 h / 131 °C
View Scheme
参考文献
Buechi, George; Botkin, James H.; Lee, Gary C. M.; Yakushijin, Kenichi
Journal of the American Chemical Society, 1985 , vol. 107, # 19 p. 5555 - 5556
反应条件
caesium carbonate; allyl bromide in DMF (N,N-dimethyl-formamide)
T=20°C; 24.3 h; Stirring;
参考文献
SmithKline Beecham Corporation
Patent: US6670388 B1, 2003 ;
Location in patent: Page column 6 ;
US 6670388 B1
