Trifluoroacetic acid → (S)-6-(piperidin-3-yloxy)-2H-isoquinolin-1-one

Participants

Reaction Steps

(S)-3-(Oxo-1,2-dihydroisoquinolin-6-yloxy)piperidine-1-carboxylic acid tert-butyl ester (1.25 g, 3.6 mmol) was mixed with dichloromethane (30 ml) and trifluoroacetic acid (10 ml) at ambient temperature for 15 minutes. Volatiles were removed under reduced pressure and excess trifluoroacetic acid was azeotroped with toluene. The residue was dissolved in methanol and purified using an SCX cartridge. Concentration gave (S)-6-(piperidin-3-yloxy)-2H-isoquinolin-1-one (450 mg, 51%), El-MS: m/z=245.4 [M+H]+.

Provenance & Evidence