반응 #70557

ord-d07c9840b9234973930b2cb4f8b36d18

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    온도the solution was heated
  2. 2
    온도at reflux for one hour
  3. 3
    온도the solution was heated
  4. 4
    온도at reflux for 16 hours
  5. 5
    온도After cooling the solution to room temperature the residue
  6. 6
    기타The aqueous layer was separated
  7. 7
    기타formed in solution
  8. 8
    여과The solid was collected by filtration
  9. 9
    기타dried under high vacuum

실험 절차

In a flask containing 3-flourobenzonitrile (Matrix Scientific, 3.0 g, 25 mmol) was added methanol (30 mL) and sodium methoxide (Aldrich, 25% by wt. in methanol, 2.83 mL, 12.4 mmol). The reaction mixture was stirred for 1.5 hours and aminoacetaldehyde dimethyl acetal (Alfa Aesar, 2.60 g, 24.8 mmol) and acetic acid (2.83 mL, 49.5 mmol) were subsequently added and the solution was heated at reflux for one hour. After cooling to room temperature, methanol (25 mL) and 6 N HCl (8 mL) was added and the solution was heated at reflux for 16 hours. After cooling the solution to room temperature the residue was taken up in a 1:1 mixture (v/v) of water and ethyl acetate (50 mL). The aqueous layer was separated and the pH of this solution was adjusted to pH 9 with 2 N NaOH, upon which a white precipitate formed in solution. The solid was collected by filtration and dried under high vacuum to provide 2-(3-fluorophenyl)-1H-imidazole as an off-white solid (1.67 g, 41% yield, MS (ESI+) m/z 163.1 (M+1).

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US08536185B2uspto-grants-2013_09