[(S)-1-(6-Fluoro-2,3,4,5-tetrahydro-1H-benzo[b]azepin-9-ylcarbamoyl)ethyl]carbamic acid tert-butyl ester → [(S)-1-(5-fluoro-6,7,8,9-tetrahydro-2,9a-diazabenzo[cd]azulen-1-yl)ethyl]carbamic acid tert-butyl ester

Participants

Reaction Steps

A solution of [(S)-1-(6-fluoro-2,3,4,5-tetrahydro-1H-benzo[b]azepin-9-ylcarbamoyl)ethyl]carbamic acid tert-butyl ester (270 mg, 0.768 mmol) in AcOH (4 mL) was stirred at 80° C. for 1 h, then concentrated in vacuo. The residue was purified by column chromatography (Si—PCC, gradient 30-60% EtOAc in cyclohexane) affording the title compound as a pale pink gum (252.6 mg, 99%). LCMS (Method B): RT 2.63 min [M+H]+ 334

Provenance & Evidence