96558-78-0, A common heterocyclic compound, 96558-78-0, name is 3-Bromo-5-chlorophenylamine, molecular formula is C6H5BrClN, 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 compound A (1 g, 4.8 mmol, 1 eq ), compound B (1.2 g, 7.3 mmol, 1.5 eq ) and K2CO3 (2.0 g, 14.5 mmol, 3 eq) in 5 mL of dioxane and 1 mL of H2O was added Pd(dppf)Cl2 (354.4 mg, 484.3 pmol, 0.1 eq) under N2. The mixture was stirred at 100C for 12 hours. Then it was partitioned between 30 mL of water and 60 mL of ethyl acetate. The organic phase was separated, washed with 30 mL of brine, dried over Na2SC>4, filtered and concentrated under reduced pressure to give the crude product, which was purified by column chromatography (S1O2, eluting with a gradient of petroleum ether: ethyl acetate = 1 :0 to 1 : 1) to give 440 mg of compound C (2.6 mmol, 54.2% yield) as a brown oil.
The synthetic route of 3-Bromo-5-chlorophenylamine has been constantly updated, and we look forward to future research findings.
Reference:
Patent; AQUINNAH PHARMACEUTICALS, INC.; VACCA, Joseph, P.; WAGER, Travis, T.; (383 pag.)WO2020/117877; (2020); A1;,
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