反应详情

To a solution of [(S)-1-(5-bromo-2-methoxy-naphthalen-1-ylmethyl)-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepin-3-yl]-carbamic acid tert-butyl ester (Intermediate 5) (480 mg, 0.913 mmol) in DCM (8 mL) at 0° C. was added TFA (1.9 mL) dropwise. The mixture was stirred for 2 h at RT and evaporated. The residue was triturated with hexane to afford (S)-3-amino-1-(5-bromo-2-methoxy-naphthalen-1-ylmethyl)-1,3,4,5-tetrahydro-benzo[b][1,4]diazepin-2-one trifluoroacetate (260 mg) as brown solid. LC-MS: 428 (M+H).

1. customevaporated
2. customThe residue was triturated with hexane