Extracurricular laboratory: Synthetic route of 2-Bromo-5-chloroaniline

According to the analysis of related databases, 2-Bromo-5-chloroaniline, the application of this compound in the production field has become more and more popular.

823-57-4, In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 823-57-4 as follows.

A 10 L round-bottom flask was charged with 200 g (1.64 mol, 1.05 eq.) of Phenylboronic acid, 322 g (1.56 mol, 1 eq.) of 2-bromo-5-chloroaniline, 90 g (78.10 mmol, 0.05 eq.) of Pd(PPh3)4, and 646 g (4.69 mol, 3 eq.) of K2CO3, after which toluene/EtOH/H2O was added thereto, and the mixture was stirred under reflux. After completion of the reaction, the mixture was extracted with MC/H2O and the MC layer was dried over MgSO4. Purification was performed using a silica-gel column to obtain 254 g of Core 1-1 at a yield of 80percent.

According to the analysis of related databases, 2-Bromo-5-chloroaniline, the application of this compound in the production field has become more and more popular.

Reference:
Patent; SOULBRAIN CO., LTD.; HA, Jong Jin; YOO, Hyun Young; KIM, Sung Soo; LEE, Seok Jong; (103 pag.)US2019/161485; (2019); A1;,
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