反応 #53990

ord-f111c92c1d8f42b1bfcc3068d7013a61

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    抽出The aqueous layer was extracted with ethyl acetate (3×75 mL)
  2. 2
    洗浄The combined extracts were washed with saturated sodium chloride
  3. 3
    乾燥dried over sodium sulfate
  4. 4
    ろ過filtered
  5. 5
    濃縮concentrated in vacuo
  6. 6
    その他The resultant residue was chromatographed (flash column, silica gel, 5% methanol in methylene chloride)

実験手順

To a solution of tert-butyl (5S,12S)-12-[(R)-[(3R,4R,5R)-3,4-bis{[tert-butyl(dimethyl)silyl]oxy}-5-(3-(4-methoxybenzyl)-2,4-dioxo-3,4-dihydro-1(2H)-pyrimidinyl)tetrahydro-2-furanyl](hydroxy)methyl]-5-isobutyl-3,6-dioxo-1-phenyl-2-oxa-4,7,11-triazatridecan-13-oate (420 mg, 0.409 mmol, obtained from Example 4) in acetonitrile (20 ml) was added a solution of ammonium cerium(IV) nitrate (898 mg, 1.6 mmol) in water (4 ml). The resulting solution was stirred for 48 hours at room temperature, and saturated sodium chloride aqueous solution was added. The aqueous layer was extracted with ethyl acetate (3×75 mL). The combined extracts were washed with saturated sodium chloride, dried over sodium sulfate, filtered and concentrated in vacuo. The resultant residue was chromatographed (flash column, silica gel, 5% methanol in methylene chloride) to provide tert-butyl (5S,12S)-12-[(R)-[(3R,4R,5R)-3,4-bis{[tert-butyl(dimethyl)silyl]oxy}-5-(2,4-dioxo -3,4-dihydro-1(2H)-pyrimidinyl)tetrahydro-2-furanyl](hydroxy)methyl]-5-isobutyl-3,6-dioxo-1-phenyl-2-oxa-4,7,11-triazatridecan-13-oate (91 mg, 25%) as a pale tan amorphous solid.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US06858591B2uspto-grants-2005_02