321-50-6

基本信息
4-氟靛紅酸酐
7-氟-2H-3,1-苯并噁嗪-2,4-二酮
7-氟-1H-苯并[D][1,3]惡嗪-2,4-二酮
7-氟-2H-3,1-苯并惡嗪-2,4(1H)-二酮
FLUOROBENZOXAZINEDIONE
7-Fluoroisatoic anhydride
7-fluoro-1H-3,1-benzoxazine-2,4-dione
7-FLUORO-2H-3,1-BENZOXAZINE-2,4(1H)-DIONE
7-Fluoro-1H-benzo[d][1,3]oxazine-2,4-dione
2H-3,1-Benzoxazine-2,4(1H)-dione, 7-fluoro-
7-fluoro-2,4-dihydro-1H-3,1-benzoxazine-2,4-dione
7-Fluoro-2H-3,1-benzoxazine-2,4(1H)-dione, 7-Fluoro-1H-benzo[d][1,3]oxazine-2,4-dione
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
制備方法

32315-10-9

446-32-2

321-50-6
步驟A-中間體化合物Int-4a的合成:在0℃下,向2-氨基-4-氟苯甲酸(15.5g,100mmol)的四氫呋喃(THF,200mL)溶液中緩慢加入三光氣(27.9g,105mmol)。將反應(yīng)混合物升溫至50℃,持續(xù)攪拌6小時(shí)。反應(yīng)完成后,通過(guò)減壓蒸餾去除溶劑。所得粗產(chǎn)物用乙酸乙酯/石油醚(1:1,v/v)混合溶劑研磨,過(guò)濾收集固體,得到中間體化合物Int-4a(15.7g,收率85%)。產(chǎn)物經(jīng)1H NMR(400 MHz,DMSO-d6)表征:δ 11.9(s,1H),7.95-7.98(m,1H),7.06-7.11(m,1H),6.84-6.89(m,1H)。
參考文獻(xiàn):
[1] Patent: WO2014/11769, 2014, A1. Location in patent: Page/Page column 35
[2] Patent: WO2014/8636, 2014, A1. Location in patent: Page/Page column 35
[3] Patent: US2015/203512, 2015, A1. Location in patent: Paragraph 0191; 0192
[4] Journal of Medicinal Chemistry, 2006, vol. 49, # 3, p. 971 - 983
[5] Patent: WO2010/79431, 2010, A2. Location in patent: Page/Page column 47-49