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0 °C

To a refluxing suspension of lithium aluminum hydride (16.1 g, 424 mmol, 3.50 equiv.) in dioxane (800 mL) was added a solution of 2-amino-N-(1-benzylpiperidin-4-yl)-3-fluorobenzamide (39.7 g, 121 mmol) in dioxane (250 mL) at such a rate that gas evolution was limited to a safe flow. Upon completion of the addition, the resulting suspension was heated at reflux for 4 h. The reaction was cooled to 0° C., and quenched by the cautious addition of 20% potassium hydroxide. Upon formation of a white, filterable precipitate, the solid was filtered through a course glass sintered funnel, and the eluent concentrated to give 36.3 g (96%) as a light yellow oil which was used without purification. Mass spec.: 314.29 (MH)+.

1. additionUpon completion of the addition
2. temperaturethe resulting suspension was heated
3. temperatureat reflux for 4 h
4. customquenched by the cautious addition of 20% potassium hydroxide
5. filtrationUpon formation of a white, filterable precipitate, the solid was filtered through a course glass sintered funnel
6. concentrationthe eluent concentrated
7. customto give 36.3 g (96%) as a light yellow oil which
8. customwas used without purification