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0 °C

A stirred solution of [2-(2-amino-phenyl)-ethyl]-(1-benzyl-piperidin-4-yl)-amine (0.44 g, 1.42 mmol) in tetrahydrofuran (5 mL) at 0° C. was treated with carbonyl diimidazole (0.23 g, 1.42 mmol). The reaction was stirred for 30 min at 0° C. and at reflux for 1 h. After cooling to room temperature, the solvent was evaporated and the residue purified by column to afford 100 mg (21%) of the desired product. LC/MS: tR=1.29 min, 336.34 (MH)+.

1. temperatureat reflux for 1 h
2. temperatureAfter cooling to room temperature
3. customthe solvent was evaporated
4. customthe residue purified by column