Trifluoroacetic acid → 4-(3-(Azetidin-3-YL)pyrazin-2-YL)-2-fluoro-N-methylbenzamide tris(2,2,2-trifluoroacetate)

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Reaction Steps

To a mixture of tert-butyl 3-(3-(3-fluoro-4-(methylcarbamoyl)phenyl)pyrazin-2-yl)azetidine-1-carboxylate (5.19 g, 13.43 mmol), prepared according to Step 1 of Example 8, and CH2Cl2 (20 mL) was added trifluoroacetic acid (7.24 mL, 94.00 mmol). The mixture was stirred at room temperature for 1 h. LCMS showed the product. The mixture was concentrated in vacuo. CH2Cl2 was added and evaporated to remove extra TFA. Ether was added and evaporated. The product was obtained as a yellow oil after drying on vacuum overnight and used in next step without purification. m/z=287 (M+1).

Provenance & Evidence