Реакция #40981

ord-f8171c7006b0492aa5e0fccdfb9481a4

Растворители

Условия реакции

Подробные условия
See reaction.notes.procedure_details.

Обработка

  1. 1
    Температураat reflux for 3 hours
  2. 2
    ДругоеThe solvent was evaporated under vacuum
  3. 3
    Другоеthe crude was partitioned between water and ethyl acetate
  4. 4
    СушкаThe organic phase was dried (Na2SO4)
  5. 5
    Другоеevaporated
  6. 6
    ДругоеThe crude was triturated with iPrOH

Методика

2,4-Dimethoxy-pyrimidine-5-boronic acid (966 mg, 5.3 mmol) was dissolved in degassed n-PrOH (60 ml) and then 2-bromo-6-fluoropyridine (850 mg, 4.8 mmol), Na2CO3 (1.676 g, 15.8 mmol), PPh3 (400 mg, 1.52 mmol) and Pd(OAc)2 (116 mg) were added. The suspension was stirred at reflux for 3 hours. The solvent was evaporated under vacuum and the crude was partitioned between water and ethyl acetate. The organic phase was dried (Na2SO4) and evaporated. The crude was triturated with iPrOH to give 650 mg of the title compound as a white powder (52% yield).

Источник

DOI: 10.6084/m9.figshare.5104873.v1Патент: US07727988B2uspto-grants-2010_06