Hydrochloric Acid → (S)-5'-fluoro-2-[2-(4-fluoro-phenyl)-morpholin-4-yl]-1-methyl-1H-[4,4']bipyrimidinyl-6-one

Participants

Reaction Steps

To a mixture of (S)-2-(4-fluorophenyl)-morpholine hydrochloride (0.19 g, 0.87 mmol; This compound was synthesized according to WO2007/011065) and 2-chloro-5′-fluoro-1-methyl-1H-[4,4′]bipyrimidinyl-6-one (intermediate 1, 0.20 g, 0.83 mmol) in tetrahydrofuran (5 mL) was added triethylamine (0.35 mL, 2.5 mmol) at room temperature. The reaction mixture was stirred for 8 hours and poured into 1N hydrochloric acid. Extraction with chloroform was performed and the organic phase was dried over anhydrous sodium sulfate. The organic solvent was removed under reduced pressure and the residue was crystallized from ethanol to afford (S)-5′-fluoro-2-[2-(4-fluoro-phenyl)-morpholin-4-yl]-1-methyl-1H-[4,4′]bipyrimidinyl-6-one (0.25 g, 0.65 mmol, 78%) as colorless crystalline.

Provenance & Evidence