Molecular Formula | C12H15BF2O2 |
Molar Mass | 240.05 |
Storage Condition | under inert gas (nitrogen or Argon) at 2-8°C |
Hazard Symbols | Xi - Irritant |
use | 2, 6-difluorophenylborate pinacol ester is a carboxylate derivative, which is a widely used drug intermediate. |
preparation | in a 500 mL three-mouth bottle, add 10 g 1, 3-difluoro-2-bromobenzene, 17 g isopropanol pinacol borate and 210 mL dry tetrahydrofuran, insert the thermometer, pump off the air, fill with nitrogen for protection, cool down to -78 ℃, then slowly add 36. 1 mL n-butyl lithium with a syringe, after adding, react at -78 ℃ for 5 min. Slowly raise to room temperature for 20 min, adjust to pH = 6~7 with 2 M hydrochloric acid, stir for 30 min, stand still, delaminate, separate the organic layer, extract the water layer with ethyl acetate, and merge the organic layer. The organic layer is dried with anhydrous sodium sulfate, evaporated to remove the solvent, and passed through a silica gel chromatography column to obtain 10 g of colorless oily liquid. The yield was 82.7%. |