Trifluoroacetic acid → 1-methyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepin-2-one

Participants

Reaction Steps

To a solution of 1-methyl-2-oxo-1,2,3,5-tetrahydro-benzo[e][1,4]diazepine-4-carboxylic acid tert-butyl ester (70 mg, 0.25 mmol) in dry DCM (10 mL), was added trifluoroacetic acid (0.75 mL, 3 mL/mmol). The mixture was stirred at r.t. for 1 h. After the completion of the reaction as confirmed by TLC, excess of TFA and DCM were evaporated in vacuo to afford trifluoroacetic acid salt of 1-methyl-1,3,4,5-tetrahydrobenzo[e][1,4]diazepin-2-one (70 mg, 95%) as a gummy solid which was used as such for next coupling.

Provenance & Evidence