반응 #436963

ord-e0fd581e89874e7a8632da32c57c36a2

반응 조건

온도
30°CELSIUS
상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    기타came up to room temperature
  2. 2
    기타the layers separated
  3. 3
    추출The acidic aqueous layer was extracted with two additional portions of dichloromethane
  4. 4
    건조The combined organic layers were dried over anhydrous sodium sulfate
  5. 5
    농축concentrated on a rotary evaporator
  6. 6
    기타to give a yellow oil, which
  7. 7
    기타was purified by chromatography on silica gel (10% ethyl acetate/hexane)
  8. 8
    기타to yield an orange oil, which
  9. 9
    기타was crystallized from 95% ethanol

실험 절차

To an ice-cooled solution of (1R)-1,8,8-trimethylbicyclo[3.2.1]octane-2,4-dione (0.36 g, 2.0 mmole), triethylamine (0.20 g, 2.0 mmole) and 4-(dimethylamino)pyridine (0.24 g, 2.0 mmole) in dry dichloromethane (25 mL) was added a solution of 4-nitrophenyl isocyanate (0.33 g, 2.0 mmole) in dry dichloromethane (5 mL). The resulting mixture was allowed to stir overnight under a nitrogen atmosphere, during which time it came up to room temperature, and then was heated at 30° C. for 24 hours. The reaction mixture was treated with 2N aqueous HCl and the layers separated. The acidic aqueous layer was extracted with two additional portions of dichloromethane. The combined organic layers were dried over anhydrous sodium sulfate and concentrated on a rotary evaporator to give a yellow oil, which was purified by chromatography on silica gel (10% ethyl acetate/hexane) to yield an orange oil, which was crystallized from 95% ethanol to yield the title compound as an off-white solid (0.20 g, 30% yield), mp=168–170° C.; MS (−) ESI m/z=343 (M−H)−; [α]D25=+29.4° (c=1, DMSO).

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US07179943B2uspto-grants-2007_02