Trifluoroacetic acid → 1-[2-(1,3-Dihydro-1-oxo-5-isobenzofuranyl)ethyl]-2-piperazinone

Participants

Reaction Steps

To a flask charged with Ethyl[(2-{(tert-butoxycarbonyl)[2-(1-oxo-1,3-dihydro-2-benzofuran-5-yl)ethyl]amino}ethyl)amino]acetate (280 mg, 0.69 mmol) and a stir bar was added TFA (2 mL). The mixture was allowed to stir at RT for 1 hour. The solvent was removed under vacuum, and the residue was dissolved in EtOH (5 mL). To the solution was added Hunig's base (0.36 mL, 2.1 mmol), and the solution was heated to 150° C. in a microwave tube for 45 minutes. LC showed mostly product, which was purified by silica gel chromatography (MeOH-DCM). The adduct was treated with 4N HCl to remove the BOC group and provide the title compound. LC-MS (IE, m/z): 261 [M+1]+.

Provenance & Evidence