A new synthetic route of C6H3BrClF

The synthetic route of 4-Bromo-2-chloro-1-fluorobenzene has been constantly updated, and we look forward to future research findings.

These common heterocyclic compound, 60811-21-4, name is 4-Bromo-2-chloro-1-fluorobenzene, 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. Recommanded Product: 4-Bromo-2-chloro-1-fluorobenzene

4-Bromo-2-chloro-l- fluorobenzene (1; 16 g, 76.5 mmol) was dissolved in 50 mL of THF. The reaction mixture was cooled down to -78 C. A solution of LDA in THF (2 M, 38.2 mL, 76.4 mmol) was added dropwise over 20 min. The reaction mixture was stirred at -78 C for 10 min. DMF (8.4 mL) was added dropwise. The reaction mixture was allowed to warm -20 C and quenched with 30 mL of saturated ammonium chloride aqueous solution, extracted with methyl tert- at l ether (50 mL X 3). The combined organic layers were washed with brine, dried over anhydrous Na2S04, and concentrated under reduced pressure to give crude product, which was purified by silica gel chromatography (5-10% EtO Ac/petroleum ether) to afford 8.4 g of 5-bromo-3-chloro-2-fluorobenzaldehyde (2) as white solid (yield: 46%). 1H MR (400 MHz, DMSO-i) delta 10.10 (s, 1H), 8.26 (s, 1H), 7.93 (s, 1H).

The synthetic route of 4-Bromo-2-chloro-1-fluorobenzene has been constantly updated, and we look forward to future research findings.

Reference:
Patent; KARYOPHARM THERAPEUTICS INC.; BALOGLU, Erkan; SENAPEDIS, William; SHACHAM, Sharon; (160 pag.)WO2016/100515; (2016); A1;,
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