Acetonitrile → 4-(6-Fluoro-4-iodo-pyridin-3-ylmethyl)-morpholine

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Reaction Conditions

Reaction Steps

In a flask, combine 5-bromomethyl-2-fluoro-4-iodo-pyridine (6.13 g, 19.40 mmol), morpholine (3.38 g, 38.80 mmol) and dry CH3CN (100 mL) under nitrogen. Add N,N-diisopropylethylamine (6.76 mL, 38.80 mmol, 2 M THF solution). Heat at 81° C. for 2 hours and cool to room temperature. Dilute with dichloromethane and wash with water and saturated aqueous sodium chloride. Separate the organic layer from the aqueous layer and dry over magnesium sulfate. After filtration, concentrate in vacuo to give the crude title compound 6.23 g (99.7%). MS (ES) m/z 323 [M+1]+.

Provenance & Evidence