N-Methylethylamine → (S)-3-(1-{4-[4-(4-Ethoxy-phenyl)-piperidin-1-yl]-phenyl}-ethyl)-1-ethyl-1-methyl-urea

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Reaction Steps

To 36 mg (0.10 mmol) (S)-1-{4-[4-(4-ethoxy-phenyl)-piperidin-1-yl]-phenyl}-ethylamine hydrochloride (XII.1) in 1.5 mL 1,4-dioxane are added 37 μL (0.25 mmol) DBU and 33 mg (0.20 mmol) CDT. The mixture is stirred for 5 min at rt. Subsequently 7.1 mg (0.12 mmol) ethyl-methyl-amine in 1.0 mL 1,4-dioxane are added and stirring is continued for 12 h at rt. The solvent is removed under reduced pressure, the residue is taken up in DMF and purified by HPLC (Sunfire, narrow gradients, water (+0.1% TFA)/methanol) to yield the desired product.

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