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Questions And Answer

• Synthesis

  In a 500 mL three-necked flask, 10 g of 1,3-difluoro-2-bromobenzene, 17 g of isopropanol pinacol boronic acid ester, and 210 mL of dry tetrahydrofuran were added. A thermometer was inserted, air was evacuated, and nitrogen was applied for protection. The temperature was lowered to -78 °C. Then, 36.1 mL of n-butyllithium was slowly added using a syringe. After the addition was complete, the mixture was reacted at -78 °C for 5 min. The temperature was then slowly raised to room temperature and reacted for 20 min. The pH was adjusted to 6-7 with 2 M hydrochloric acid, and the mixture was stirred for 30 min. After standing, the layers were separated. The organic layer was separated, and the aqueous layer was extracted with ethyl acetate. The organic layers were combined. The organic layer was dried over anhydrous sodium sulfate, the solvent was evaporated, and the mixture was filtered through a silica gel column to obtain 10 g of a colorless oily liquid. The yield was 82.7%.

  

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• Uses

  Pinaryl 2,6-difluorophenylboronic acid is a carboxylic acid ester derivative, which is a widely used pharmaceutical intermediate.;

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