Synthesis
The general procedure for the synthesis of 2-bromo-4-fluoroaniline from 4-fluoroaniline was as follows: 200 mL of distilled N,N-dimethylformamide (DMF) and 4-fluoroaniline (8.64 mL, 58.13 mmol) were added to a two-necked flask equipped with a stirring device. N-bromosuccinimide (11.4 g, 63.95 mmol) dissolved in DMF was added slowly and dropwise with stirring. After completion of the reaction, extraction was carried out using dichloromethane (CH2Cl2). The product was purified by column chromatography (eluent ratio of ethyl acetate: n-hexane = 1:4), and the target product 2-bromo-4-fluoroaniline was finally obtained in 95% yield.
References
[1] Patent: KR2018/50795, 2018, A. Location in patent: Paragraph 0134; 0135; 0152-0154
[2] Tetrahedron Letters, 2000, vol. 41, # 13, p. 2083 - 2085
[3] Journal of the American Chemical Society, 2011, vol. 133, # 18, p. 6868 - 6870
[4] Chemistry - A European Journal, 2011, vol. 17, # 49, p. 13665 - 13669
[5] Tetrahedron Letters, 2014, vol. 55, # 38, p. 5338 - 5341
