Trifluoroacetic acid → (1S,9S)-9-(benzyloxycarbonylamino)-6,10-dioxo octahydro-1H-pyridazino[1,2-a][1,2]diazepine-1-carboxylic acid

Participants

Reaction Steps

In a 10 mL round-bottomed flask, (1S,9S)-tert-butyl 9-(benzyloxycarbonylamino)-6,10-dioxooctahydro-1H-pyridazino[1,2-a][1,2]diazepine-1-carboxylate (1.3 g, 3.01 mmol) was combined with CH2Cl2 (5 ml) to give a colorless solution. TFA (3.53 g, 2.38 ml, 31.0 mmol) was added and stirred at room temperature for 5 hr. The crude reaction mixture was concentrated in vacuo and redissolved in EtOAc (10 ml). It was evaporated to afford (1S,9S)-9-(benzyloxycarbonylamino)-6,10-dioxooctahydro-1H-pyridazino[1,2-a][1,2]diazepine-1-carboxylic acid as a foaming solid (1.0 g, 88.4%).

Provenance & Evidence