6-氟吲唑作为医药中间体或活性成分,用于相关药物研发与生产。
医药
路线1:
- 步骤: 以5-氟-2-甲基苯胺(3g,0.024mol)为原料,与乙酸钾(2.8g,0.028mol)和乙酸酐(6.8mL,0.072mol)在氯仿(30mL)中混合,40℃加热0.5小时;加入异戊酸硝酸酯(3.8mL,0.028mol),升温至80℃静置反应12小时;减压蒸馏除溶剂,残余物用碳酸钠水溶液碱化,乙酸乙酯萃取;有机层经水和盐水洗涤,减压浓缩得粗产物;硅胶柱色谱(30%乙酸乙酯/己烷)纯化;纯化合物用甲醇盐酸溶液(60mL)处理30分钟,减压浓缩后碱化,乙酸乙酯萃取,有机层洗涤干燥浓缩;柱色谱(正己烷/乙酸乙酯=7:3)纯化。
- 收率: 2.0g,62%。
- 参考文献: [1] Patent: WO2015/104662, 2015, A1. Location in patent: Page/Page column 37; 38;[2] Patent: US2016/326151, 2016, A1. Location in patent: Paragraph 0206;[3] Bioorganic and Medicinal Chemistry, 2008, vol. 16, # 4, p. 1966 - 1982;[4] Bioorganic and Medicinal Chemistry Letters, 2007, vol. 17, # 11, p. 3177 - 3180;[5] Bioorganic and Medicinal Chemistry, 2004, vol. 12, # 9, p. 2115 - 2137