تفاعل #719655

معادلة التفاعل

HCl

4-borono-2-fluorobenzoic acid

HATU

morpholine

→

crude compound

المردود 87.3%

(3-Fluoro-4-(morpholine-4-carbonyl)phenyl) boronic acid

المردود 87.3%

المذيبات

DMF

ظروف التفاعل

المعالجة

1. 1
   workup.ADDITIONThe reaction mixture was poured into ice cold water
2. 2
   استخلاصextracted with EtOAc (2×50 mL)
3. 3
   غسيلThe organic layer was washed with brine solution (20 mL)
4. 4
   تجفيفdried over anhydrous Na2SO4 and solvent
5. 5
   أخرىwas evaporated under reduced pressure

الإجراء التجريبي

To a solution of 4-borono-2-fluorobenzoic acid (1.0 g, 5.43 mmol) and HATU (2.0 g, 5.43 mmol) in DMF (20.0 mL) was added morpholine (0.9 g, 10.87 mmol) at room temperature. The reaction mixture was stirred at room temperature for 18 h. The reaction mixture was poured into ice cold water, acidified with 1N HCl, extracted with EtOAc (2×50 mL). The organic layer was washed with brine solution (20 mL), dried over anhydrous Na2SO4 and solvent was evaporated under reduced pressure to afford 1.2 g of crude compound as a colourless gum. Crude compound was directly used for the next step without any further purification.

المصدر