105391-70-6

基本信息
5-溴-6-氟-1H-吲唑 1G
5-BROMO-6-FLUOROINDAZOLE
5-BROMO-6-FLUORO-1H-INDAZOLE
1H-Indazole, 5-bromo-6-fluoro-
物理化学性质
制备方法

633335-81-6

105391-70-6
以1-(5-溴-6-氟-1H-吲唑-1-基)乙酮为原料合成5-溴-6-氟-1H-吲唑的一般步骤:将1-(5-溴-6-氟-1H-吲唑-1-基)乙酮(1.58 g,6.15 mmol)溶于3M HCl水溶液(20 mL)和甲醇(4 mL)的混合溶剂中。将反应混合物在90℃下加热回流3小时。反应完成后,冷却至室温,用1M NaOH水溶液调节pH至10。此时,溶液中析出无色固体,过滤收集固体,并用真空干燥,得到目标产物5-溴-6-氟-1H-吲唑(1.22 g,收率93%)。产物的1H NMR(CDCl3)数据如下:δ 9.0-10.20(1H,br),8.02(1H,s),7.97(1H,d,J = 6.4 Hz),7.28(1H,s)。
参考文献:
[1] Patent: WO2012/103806, 2012, A1. Location in patent: Page/Page column 55
[2] Patent: WO2006/44860, 2006, A2. Location in patent: Page/Page column 37-38
[3] Patent: US2016/347717, 2016, A1. Location in patent: Paragraph 0619; 0620
[4] Patent: WO2009/32123, 2009, A2. Location in patent: Page/Page column 179-180
[5] Patent: WO2009/32125, 2009, A1. Location in patent: Page/Page column 119