Reference of 115843-99-7, These common heterocyclic compound, 115843-99-7, name is 4-Bromo-3-chloro-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 solution of 4-bromo-3-chloro-2-fluoro-aniline (3 g, 13.4 mmol) and HATU (10.2 g, 26.7 mmol) in DMA (30 mL) was added TEA (5.58 mL, 40.1 mmol) and 3-tert-butoxy-3-oxopropanoic acid (3.09 mL, 20.0 mmol) at RT. The mixture was stirred at 50 C for 1 h, diluted with water, and extracted with EtOAc. The organic layer was washed with brine, dried over anhydrous Na 2SO 4, filtered, and concentrated in vacuo. The residue was purified by column chromatography on silica gel (gradient elution, 30 – 70% EtOAc/hexane) to give tert-butyl 3-(4-bromo-3-chloro-2-fluoro-anilino)-3-oxo-propanoate (3.35 g).
Statistics shows that 4-Bromo-3-chloro-2-fluoroaniline is playing an increasingly important role. we look forward to future research findings about 115843-99-7.
Reference:
Patent; TAIHO PHARMACEUTICAL CO., LTD.; OTSUKA PHARMACEUTICAL CO., LTD.; SHIMAMURA, Tadashi; KATO, Ryo; MIURA, Risako; MITA, Takashi; OGAWA, Takahiro; SAGARA, Yufu; JOHNSON, Christopher Norbert; HOWARD, Steven; DAY, James Edward Harvey; ST. DENIS, Jeffrey David; LIEBESCHUETZ, John Walter; (345 pag.)WO2020/22323; (2020); A1;,
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