反应详情

A solution of 26 mg of N-[(S)-1-(2-benzyloxy-ethyl)-4-oxo-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepin-3-yl]-2-hydroxy-2-methyl-N′-(2,2,3,3,3-pentafluoro-propyl)-malonamide in 2.0 ml of methanol was treated with 10 mg of palladium on carbon (10%) and stirred for 3 days under an atmosphere of hydrogen. During this period of time, the catalyst was replaced three times after filtration of the reaction mixture over Dicalit. For the final working-up, the reaction mixture was filtrated over Dicalit and the solvent evaporated under reduced pressure. After separation of mainly unchanged starting material by chromatography on silica gel using a gradient of heptane/ethyl acetate=100/0 to 20/80 as the eluent, 6 mg (29% of theory) of the title compound were obtained as a white foam; MS (m/e): 469 (M+H)+.

1. waitDuring this period of time
2. filtrationafter filtration of the reaction mixture over Dicalit
3. filtrationFor the final working-up, the reaction mixture was filtrated over Dicalit
4. customthe solvent evaporated under reduced pressure
5. customAfter separation
6. customwere obtained as a white foam