119023-25-5

基本信息
2-氨基-4-氟苯甲酰胺
4-fluoroanthranilaMide
2-Amino-4-fluorobenzamide
Benzamide, 2-amino-4-fluoro-
Benzamide, 2-amino-4-fluoro- (9CI)
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
制備方法

446-32-2

119023-25-5
步驟A:在氮?dú)獗Wo(hù)下,將2-氨基-4-氟苯甲酸(4.0g,25.8mmol)溶解于脫氣的DMF(50mL)中。依次加入HOBt(4.19g,31mmol)、DIEA(5.4mL,31mmol)、EDCI(5.94g,31mmol)和2N氨的甲醇溶液(18mL,36.1mmol)。將反應(yīng)混合物在室溫下攪拌48小時(shí)。反應(yīng)完成后,在減壓下濃縮反應(yīng)液。殘余物通過(guò)硅膠柱色譜法純化,得到2-氨基-4-氟苯甲酰胺,為白色固體(2.89g,產(chǎn)率66%)。1H NMR(300MHz,DMSO-d6)δ6.28(m,1H),6.44(m,1H),6.90(br s,2H),7.08(m,1H),7.58(m,1H),7.71(br d,1H)。
參考文獻(xiàn):
[1] Patent: WO2010/99379, 2010, A1. Location in patent: Page/Page column 135
[2] Patent: WO2018/125961, 2018, A1. Location in patent: Page/Page column 58; 59
[3] Bioorganic and Medicinal Chemistry, 2000, vol. 8, # 3, p. 497 - 506
[4] Patent: US2014/275072, 2014, A1. Location in patent: Paragraph 0132; 0133
[5] Journal of Agricultural and Food Chemistry, 2015, vol. 63, # 31, p. 6883 - 6889