1,2-Diaminocyclohexane, trans- → 1-Benzothiazol-6-yl-3-[4-(1-hydroxyethyl)-pyridin-3-yl]-imidazolidin-2-one

Participants

Reaction Steps

Using the same reaction conditions as described in example 14, 1-benzothiazol-6-yl-imidazolidin-2-one (I-84b: 150 mg, 0.6849 mmol) was reacted with 1-(3-bromo-pyridin-4-yl)-ethanol (137.6 mg, 0.6849 mmol), 1,4-dioxane (5 mL), copper iodide (13.04 mg, 0.06849 mmol), trans-1,2-diamino cyclohexane (23.52 mg, 0.205 mmol) and potassium phosphate (435.1 mg, 2.05 mmol) to afford the crude product. Purification by column chromatography on silica gel (2% MeOH in CHCl3), followed by preparative HPLC afforded 9 mg of the product (3.9% yield).

Provenance & Evidence