Trifluoroacetic acid → 5-[4-(azetidin-3-yloxy)-3-methoxy-phenyl]-2-(4-chloro-phenyl)-6,7-dihydro-5H-thiazolo[5,4-c]pyridin-4-one

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Reaction Steps

Dissolve 3-{4-[2-(4-chloro-phenyl)-4-oxo-6,7-dihydro-4H-thiazolo[5,4-c]pyridin-5-yl]-2-methoxy-phenoxy}-azetidine-1-carboxylic acid tert-butyl ester (2.71 g, 5.00 mmol) in CH2Cl2 (20 mL). Add trifluoroacetic acid (5.88 mL, 77.79 mmol). Stir at room temperature for one hour and then add 5 N NaOH to pH=8-10. Collect a white/yellow precipitate via vacuum filtration, and wash the solid with EtOAc followed by Et2O. Dry the solid overnight in vacuo at about 50° C. to give 2.21 g (>99%) of the title compound. ES/MS m/z (35Cl) 442.0 [M+1]+.

Provenance & Evidence