Reference of 58534-95-5, These common heterocyclic compound, 58534-95-5, name is 3-Bromo-2-fluoroaniline, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
To a stirred solution of N-Boc-trans-4-fluoro-proline (25 g, 1 equiv), 3-bromo-2- fluoroaniline (14.5 mL, 1.2 equiv) and HATU (53 g, 1.3 equiv) in DMF (250 mL) was added DIPEA (37 mL, 2 equiv) and the resulting solution was stirred at room temperature under an atmosphere of nitrogen. The reaction mixture was poured into water and filtered and the collected solid was washed with excess water. The solid was dissolved in DCM and washed with 10% NaHCCb, 1.5 N HC1, and brine. The solvent was removed under vacuum, hexane was added, and the precipitated solid was collected by filtration to afford the title product (27 g).
Statistics shows that 3-Bromo-2-fluoroaniline is playing an increasingly important role. we look forward to future research findings about 58534-95-5.
Reference:
Patent; ACHILLION PHARMACEUTICALS, INC.; WILES, Jason, Allan; PHADKE, Avinash, S.; DESHPANDE, Milind; AGARWAL, Atul; CHEN, Dawei; GADHACHANDA, Venkat, Rao; HASHIMOTO, Akihiro; PAIS, Godwin; WANG, Qiuping; WANG, Xiangzhu; GREENLEE, William; (447 pag.)WO2017/35408; (2017); A1;,
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