Toluene → (S)-1-(5-Fluoro-6,7,8,9-tetrahydro-2,9a-diazabenzo[cd]azulen-1-yl)ethylamine

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Reaction Steps

To an ice-cooled solution of [(S)-1-(5-fluoro-6,7,8,9-tetrahydro-2,9a-diazabenzo[cd]azulen-1-yl)ethyl]carbamic acid tert-butyl ester (252.6 mg, 0.7576 mmol) in DCM (8 mL) was added TFA (2 mL) and the mixture was stirred at RT for 1.5 h. Toluene was added and volatiles were removed under reduced pressure, the resulting residue was dissolved in MeOH and loaded onto an Isolute® SCX-2 cartridge. The cartridge was washed with MeOH and the product was eluted with 0.5M NH3/MeOH. The product containing fractions were combined and concentrated in vacuo affording the title compound as a light pink solid (144.5 mg, 82%). LCMS (Method J): RT 1.93 min [M+H]+ 234

Provenance & Evidence