Ethylenediamine → 4-(2-Aminoethyl)-1-(4-trifluoromethylpyrimidin-2-yl)-piperidin-4-ol

Participants

Reaction Steps

The process is performed according to the procedure described in Example 1 (step 1.4.). Starting with 0.38 g (0.68 mmol) of 4,5,6,7-tetrachloro-2-{2-[4-hydroxy-1-(4-trifluoromethylpyrimidin-2-yl)piperidin-4-yl]ethyl}isoindole-1,3-dione), obtained in the preceding step, dissolved in an acetonitrile/tetrahydrofuran/water mixture (2/1/1) and 0.18 g (3.06 mmol) of ethylenediamine in 4.50 mL of ethanol, and after chromatography on silica gel, eluting with a 90/10/1 mixture of dichloromethane, methanol and 28% aqueous ammonia, 0.15 g of expected product is obtained in the form of a wax.

Provenance & Evidence