반응 #217681

ord-f870bbdbea3f49b08af61cd495e4b3df

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    온도cooling under a nitrogen atmosphere
  2. 2
    workup.ADDITIONwere added dropwise
  3. 3
    workup.STIRRINGat −75° C., and the mixture was stirred for 25 minutes at ice-
  4. 4
    온도cooling
  5. 5
    여과after the solids were filtered off
  6. 6
    농축the filtrate was concentrated under reduced pressure
  7. 7
    기타the residue was purified by column chromatography (silica gel: Wako gel C200, eluent: hexane-ethyl acetate=5:1)

실험 절차

48 μL of pyridine and 78 μL of trifluoromethane sulfonic acid anhydride dissolved in 0.4 mL of dichloromethane were added dropwise to 120 mg of (1R,2R,3R,5R,6R)-2-azido-6-fluoro-3-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid diethyl ester dissolved in 20 mL of dichloromethane at −75° C., and the mixture was stirred for 1.5 hours at ice-cooling under a nitrogen atmosphere. 24 μL of pyridine and 39 μL of trifluoromethane sulfonic acid anhydride dissolved in 0.2 mL of dichloromethane were added dropwise thereto at −75° C., and the mixture was stirred for 25 minutes at ice-cooling. 10 mL of ether was added thereto, and after the solids were filtered off, the filtrate was concentrated under reduced pressure, and the residue was purified by column chromatography (silica gel: Wako gel C200, eluent: hexane-ethyl acetate=5:1), thereby yielding 166 mg of (1R,2R,3R,5R,6R)-2-azido-6-fluoro-3-trifluoromethanesulfonyloxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic acid diethyl ester.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US07381746B2uspto-grants-2008_06