Reference of 96558-78-0, In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 96558-78-0 as follows.
To a solution of 3-bromo-5-chloro-aniline (150 mg, 726.5 pmol, 1 eq ), 4-pyridylboronic acid (107.2 mg, 871.9 pmol, 1.2 eq) and K2CO3 (200.9 mg, 1.5 mmol, 2 eq) in 2 mL of dioxane and 0.2 mL of H2O was added Pd(dppf)Cl2 (53.2 mg, 72.7 pmol, 0.1 eq) and purged with N2 for 3 times. The mixture was stirred at 100C for 12 hour. The reaction mixture was partitioned between 15 mL of water and 25 mL of ethyl acetate. The organic phase was separated, washed with 15 mL of brine, dried over Na2SC>4, filtered and concentrated under reduced pressure to give the crude product, which was purified by prep- TLC (S1O2, eluting with a gradient of petroleum ether:ethyl acetate =1 : 1) to give 79 mg of compound 2 (386.0 pmol, 53.1% yield) as a yellow solid.
According to the analysis of related databases, 96558-78-0, the application of this compound in the production field has become more and more popular.
Reference:
Patent; AQUINNAH PHARMACEUTICALS, INC.; VACCA, Joseph, P.; WAGER, Travis, T.; (383 pag.)WO2020/117877; (2020); A1;,
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