反应详情

A mixture of (5S,7S)-5-(4-cyanobenzyl)-3-(3,5-dichlorophenyl)-7-amino-1,3-diazabicyclo[3.3.0]octane-2,4-dione (200 mg), malonamic acid (59.5 mg), EDC (112 mg), HOBT (97.5 mg) and DIEA (168 μL) in THF (5 mL) was stirred overnight at room temperature. The reaction mixture was evaporated. The residue was dissolved in EtOAc and the resulting solution was washed with water, saturated aqueous NaHCO3 solution, brine, dried (Na2SO4) and concentrated to give 212 mg of the titled compound. MS (m/z) 500 (MH+).

1. customThe reaction mixture was evaporated
2. dissolutionThe residue was dissolved in EtOAc
3. washthe resulting solution was washed with water, saturated aqueous NaHCO3 solution, brine
4. dry with materialdried (Na2SO4)
5. concentrationconcentrated