Some common heterocyclic compound, 452-74-4, name is 1-Bromo-2-fluoro-4-methylbenzene, molecular formula is C7H6BrF, 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. Quality Control of 1-Bromo-2-fluoro-4-methylbenzene
1-Bromo-4-(bromomethyl)-2-fluorobenzene: In a flame dried round-bottomed flask equipped with a magnetic stir bar and under inert atmosphere (N2), a solution of commercially available 1-bromo-2-fluoro-4-methylbenzene (1.37 mL, 106 mmol) in AcCN (25 mL) was treated with /V-bromosuccinimide (2.83 g, 15.9 mmol) and the reaction mixture was heated to 80 C before to add benzoyl peroxide (2.73 mg, 8.46 mmol) and the reaction mixture was stirred for 1.5 h at 80 C. The reaction mixture was partitioned between water (30 mL) and EA (20 mL). The org. layer was washed with brine, dried over MgS04, filtered, and the solvent was removed under reduced pressure. Purification of the residue by FC (1 : 19? 1 : 10 EA/hept) gave the title compound as yellow oil: TLC: rf (1 :10 EA/hept) = 0.58. LC-MS-conditions 07: tR = 0.91 min.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 452-74-4, its application will become more common.
Reference:
Patent; ACTELION PHARMACEUTICALS LTD; CORMINBOEUF, Olivier; CREN, Sylvaine; LEROY, Xavier; POZZI, Davide; WO2015/19325; (2015); A1;,
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