4-氟-苯并[d]异噁唑-3-醇合成路线 （共 5 条）
反应条件
1: With 1,1'-carbonyldiimidazole in tetrahydrofuran
T=25 - 60°C; 7 h;
2: With hydrogenchloride in tetrahydrofuran; water
T=15 - 20°C; pH=1; 1.25 h;
参考文献
PFIZER INC.; NOGUCHI, Hirohide; WAIZUMI, Nobuaki
Patent: WO2011/101774 A1, 2011 ;
Location in patent: Page/Page column 25; 27 ;
参考文献
Sankyo Company, Limited
Patent: US5965591 A1, 1999 ;
反应条件
tri-iso-propylsilane; trifluoroacetic acid in dichloromethane
2 h; Inert atmosphere;
参考文献
Ferraris, Dana; Duvall, Bridget; Ko, Yao-Sen; Thomas, Ajit G.; Rojas, Camilo; Majer, Pavel; Hashimoto, Kenji; Tsukamoto, Takashi
Journal of Medicinal Chemistry, 2008 , vol. 51, # 12 p. 3357 - 3359
反应条件
1.1: sulfuric acid / 45 h / 60 °C
2.1: hydroxylammonium sulphate; potassium carbonate / water; methanol / 21.5 h / 15 - 35 °C / Industry scale
3.1: 1,1'-carbonyldiimidazole / tetrahydrofuran / 7 h / 25 - 60 °C
3.2: 1.25 h / 15 - 20 °C / pH 1
View Scheme
参考文献
PFIZER INC.; NOGUCHI, Hirohide; WAIZUMI, Nobuaki
Patent: WO2011/101774 A1, 2011 ;
反应条件
1.1: hydroxylammonium sulphate; potassium carbonate / water; methanol / 21.5 h / 15 - 35 °C / Industry scale
2.1: 1,1'-carbonyldiimidazole / tetrahydrofuran / 7 h / 25 - 60 °C
2.2: 1.25 h / 15 - 20 °C / pH 1
View Scheme
参考文献
PFIZER INC.; NOGUCHI, Hirohide; WAIZUMI, Nobuaki
Patent: WO2011/101774 A1, 2011 ;
