2-Imidazolidinone → 1-(4-Cyclopropylpyridin-3-yl)-3-(5-fluoro-3-methylbenzo[b]thiophen-6-yl)imidazolidin-2-one

Participants

Reaction Steps

Using analogous reagents and reaction conditions as described in Example 1 above, 4-cyclopropyl-pyridin-3-yl)-imidazolidin-2-one (I-1d: 150 mg, 0.7389 mmol) was reacted with 6-bromo-5-fluoro-3-methyl-benzo[b]thiophene (I-29b: 216 mg, 0.8866 mmol), 1,4-dioxane (5 mL), copper iodide (14.07 mg, 0.0738 mmol), trans-N,N′-dimethylcyclohexane-1,2-diamine (10.4 mg, 0.0.0738 mmol) and potassium phosphate (469.9 mg, 2.2167 mmol) to afford the crude product. Purification by column chromatography on silica gel (1% methanol in chloroform), followed by preparative HPLC afforded 62 mg of the product (22% yield).

Provenance & Evidence