4590-52-7

基本信息
7-氟-3,4-二氫喹啉-2(1H)-酮
7-Fluoro-3,4-dihydroquinolin-2(1H)
7-fluoro-3,4-dihydro-2(1H)-Quinolinone
7-Fluoro-3,4-dihydroquinolin-2(1H)-one
2(1H)-Quinolinone, 7-fluoro-3,4-dihydro-
物理化學性質
制備方法

100638-26-4

4590-52-7
以3-氯-N-(3-氟苯基)丙酰胺為原料合成7-氟-3,4-二氫喹啉-2(1H)-酮的一般步驟:向裝有磁力攪拌棒的經(jīng)火焰干燥的50 mL燒瓶中加入3-氯-N-(3-氟苯基)丙酰胺(10 g,49.6 mmol)和AlCl3(23.1 g,173.6 mmol)。將燒瓶置于預熱的油浴中,加熱至120-125℃,保持2小時,直至LC-MS分析顯示反應完成。反應完成后,將混合物冷卻至室溫,緩慢加入冰水淬滅反應。用EtOAc萃取反應混合物,合并有機相后依次用水和飽和鹽水洗滌。有機層用無水Na2SO4干燥,過濾后減壓濃縮,得到白色固體產(chǎn)物7-氟-3,4-二氫喹啉-2(1H)-酮(7.63 g,收率93.2%)。
參考文獻:
[1] Patent: WO2016/66597, 2016, A1. Location in patent: Page/Page column 39
[2] Patent: WO2016/86200, 2016, A1. Location in patent: Page/Page column 273; 274
[3] Patent: WO2012/94462, 2012, A2. Location in patent: Page/Page column 86
[4] Patent: CN106349241, 2017, A. Location in patent: Paragraph 0488; 0492; 0493; 0494; 0495
[5] Patent: WO2008/42735, 2008, A1. Location in patent: Page/Page column 59