Trifluoroacetic acid → (1R,6S)-8-((1R)-1-Phenyl-ethyl)-3,8-diaza-bicyclo[4.2.0]octane

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Reaction Steps

To the minor isomer product of Example 3E (9.3 g, 29.4 mmol) in 40 mL CH2Cl2 at 0° C. was added 20 mL trifluoroacetic acid. The ice bath was removed after the addition and the mixture stirred at ambient temperature for 3 h then was concentrated under reduced pressure and the residue was purified via column chromatography (SiO2, 1% NH4OH:9% CH3OH:90% CH2Cl2) to give the title compound. MS (DCl/NH3) m/z 217 (M+H)+.

Provenance & Evidence