Reaktion #44959

ord-492f2e4892ac4598ab83a5a3fb55c998

Reaktionsbedingungen

Detaillierte Bedingungen
See reaction.notes.procedure_details.

Aufarbeitung

  1. 1
    Waschenthe solution is washed successively with saturated aqueous sodium hydrogen carbonate solution, water and saturated brine
  2. 2
    Trocknendried over sodium sulfate
  3. 3
    SonstigeThe solvent is evaporated under reduced pressure
  4. 4
    SonstigeThe solid precipitates
  5. 5
    Filtrationare collected by filtration

Vorschrift

2-{[(5-Chloropyridin-2-yl)amino]carbonyl}-3-({[trans-4-(3-oxomorpholin-4-yl)cyclohexyl]carbonyl}amino)furo[3,2-b]pyridine-5-carboxylic acid (100 mg) obtained in Example 79 is dissolved in N,N-dimethylformamide (3 ml), and thereto are added successively morpholine (32 μl), 1-hydroxybenzotriazole (50 mg) and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (71 mg), and the mixture is stirred at room temperature for 15 hours. The reaction solution is diluted with ethyl acetate-tetrahydrofuran, and the solution is washed successively with saturated aqueous sodium hydrogen carbonate solution, water and saturated brine, dried over sodium sulfate. The solvent is evaporated under reduced pressure and the resulting residue is suspended in ethyl acetate-diethyl ether. The solid precipitates are collected by filtration to give the title compound (109 mg).

Quelle

DOI: 10.6084/m9.figshare.5104873.v1Patent: US07737161B2uspto-grants-2010_06