Reacción #40968

ord-49aa7eb002944783b9f978f9c7b080b9

Disolventes

Condiciones de reacción

Condiciones detalladas
See reaction.notes.procedure_details.

Tratamiento posterior

  1. 1
    Temperaturaat reflux for 4 hours
  2. 2
    OtroThe solvent was evaporated under vacuum
  3. 3
    Otrothe crude was partitioned between water and ethyl acetate
  4. 4
    SecadoThe organic phase was dried (Na2SO4)
  5. 5
    Otroevaporated
  6. 6
    OtroThe crude was purified by SCX cartridge

Procedimiento

2,4-Dimethoxy-pyrimidine-5-boronic acid (840 mg, 4.6 mmol) was dissolved in degassed n-PrOH (40 mL) and then 5-iodo-2,4-dimethyl-oxazole (Prep60, 850 mg, 3.8 mmol), Na2CO3 (848 mg, 8 mmol), PPh3 (332 mg, 1.3 mmol) and Pd(OAc)2 (85 mg, 0.38 mmol) were added. The suspension was stirred at reflux for 4 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 purified by SCX cartridge to give 600 mg of the title compound (66% yield).

Fuente

DOI: 10.6084/m9.figshare.5104873.v1Patente: US07727988B2uspto-grants-2010_06