HCID 59718717, compound → HCID 59718684, compound

Participants

Reaction Steps

A solution of 72 mg of the first eluting epimer (R or S)-N-[(S)-5-(2-benzyloxy-ethyl)-2-oxo-1-(2,2,2-trifluoro-ethyl)-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 3.0 ml of methanol was treated with 24 mg of palladium on carbon (10%) and stirred for 24 hours under an atmosphere of hydrogen. For the working-up, the reaction mixture was filtrated over Dicalit and the solvent evaporated under reduced pressure. The crude material was purified by chromatography on silica gel using a gradient of heptane/ethyl acetate=100/0 to 30/60 as the eluent, and 46 mg (79% of theory) of the title compound were obtained as a white foam; MS (m/e): 551 (M+H)+.

Provenance & Evidence