Reference of 445-02-3, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 445-02-3 name is 4-Bromo-2-(trifluoromethyl)aniline, This compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.
2-Amino-5-bromobenzotrifluoride 9a (1.1 g, 4.58 mmol), 1,2,3-propanetriol (1.69 g, 18.3 mmol) and iron (II) sulfate heptahydrate (204 mg, 0.73 mmol) were added to a reaction flask. The reaction solution was cooled to 0C, and added dropwise with 0.8 mL of sulfuric acid. After completion of the addition, the reaction solution was heated to 120C, and stirred for 4 hours. The reaction was stopped, and the reaction solution was cooled to room temperature, added with 20 mL of water, and extracted with ethyl acetate (30 mL×3). The organic phases were combined, and concentrated under reduced pressure. The residue was purified by CombiFlash rapid preparation instrument with elution system B to obtain the title product 9b (0.9 g), yield: 71.4%. MS m/z (ESI): 210.6 [M+1].
At the same time, in my other blogs, there are other synthetic methods of this type of compound, 4-Bromo-2-(trifluoromethyl)aniline, and friends who are interested can also refer to it.
Reference:
Patent; Jiangsu Hengrui Medicine Co. Ltd.; Shanghai Hengrui Pharmaceutical Co., Ltd.; LU, Biao; ZHANG, Junzhen; JIN, Fangfang; HE, Feng; TAO, Weikang; EP3569596; (2019); A1;,
Bromide – Wikipedia,
bromide – Wiktionary