Réaction #67609

ord-0bbc3258de874f4a95fa95d492a7d15b

Solvants

Conditions de réaction

Conditions détaillées
See reaction.notes.procedure_details.

Traitement

  1. 1
    workup.STIRRINGthe mixture was stirred for about 30 hours
  2. 2
    AutreThe solid which separated
  3. 3
    Filtrationwas filtered
  4. 4
    Lavagewashed with water (3×5 mL)
  5. 5
    Autredried at about 60-70° C.

Mode opératoire

To a well stirred solution of 6-(difluoromethoxy)[1]benzofuro[3,2-c]pyridine-9-carbaldehyde (500 mg, 1.90 mmol) in acetone (10 mL) was added sulphamic acid (276 mg, 2.85 mmol) at about 10° C. followed by drop wise addition of a solution of sodium chlorite (240 mg, 2.66 mmol) in water (5 mL) at about 0 to 5° C. The mixture was then stirred for about 1-2 hours. Ice cold water (50 mL) was added and the mixture was stirred for about 30 hours. The solid which separated was filtered, washed with water (3×5 mL) and dried at about 60-70° C. to give 6-(difluoromethoxy)[1]benzofuro[3,2-c]pyridine-9-carboxylic acid as a white solid.

Source

DOI: 10.6084/m9.figshare.5104873.v1Brevet: US08524905B2uspto-grants-2013_09