Ethanolamine → tert-Butyl 4-(2-hydroxyethylamino)piperidine-1-carboxylate

Beteiligte Stoffe

Reaktionsschritte

A solution of tert-butyl 4-oxo-1-piperidinecarboxylate (15 g), 2-aminoethanol (14 ml), acetic acid (6.6 ml) in 1,2-dichloroethane (300 ml) was mixed at room temperature for 1 hour, and then sodium triacetoxyborohydride (49 g) was added thereto, followed by mixing at room temperature for 15 hours. pH of the aqueous layer was adjusted to about 12 by adding a 1 N aqueous sodium hydroxide solution to the reaction mixture, and then extracted with chloroform. The extract was dried over anhydrous magnesium sulfate, and then the solvent was distilled off under reduced pressure to obtain the title compound as a colorless oil (18 g, 89%).

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