Réaction #167339

Équation de réaction

1-(4-methyl-pyridin-3-yl)-imidazolidin-2-one

4-bromo-2-fluoro-benzonitrile

trans-1,2-diamino cyclohexane

potassium phosphate

→

2-Fluoro-4-[3-(4-methyl-pyridin-3-yl)-2-oxo-imidazolidin-1-yl]-benzonitrile

Rendement 32.5%

Solvants

1,4-dioxane

Conditions de réaction

Traitement

1. 1
   Autreto afford the crude product
2. 2
   AutrePurification by column chromatography on silica gel (2% MeOH in CHCl3)

Mode opératoire

Using the same reaction conditions as in Example 14, 1-(4-methyl-pyridin-3-yl)-imidazolidin-2-one (I-14b: 300 mg, 1.693 mmol) was reacted with 4-bromo-2-fluoro-benzonitrile (372 mg, 1.86 mmol), 1,4-dioxane (50 mL), copper iodide (32.2 mg, 0.016 mmol), trans-1,2-diamino cyclohexane (61 mL, 0.5079 mmol) and potassium phosphate (900 mg, 4.23 mmol) to afford the crude product. Purification by column chromatography on silica gel (2% MeOH in CHCl3) afforded 163 mg of 2-Fluoro-4-[3-(4-methyl-pyridin-3-yl)-2-oxo-imidazolidin-1-yl]-benzonitrile (32.5% yield).

Source