General procedure for the synthesis of 1-BOC-3-hydroxymethylpiperazine from 1,4-bis(Boc)-2-piperazinemethanol: To a solution of di-tert-butyl 2-(hydroxymethyl)piperazine-1,4-dicarboxylate (4.00 g, 12.6 mmol) in ethanol (110 ml) was added sodium hydroxide (1.99 g, 49.8 mmol), and the mixture was heated under reflux conditions for 16 hours. After completion of the reaction, the solvent was removed by evaporation under reduced pressure. The residue was poured into water and the mixture was extracted with ethyl acetate and the organic phase was dried with anhydrous magnesium sulfate. The solvent was evaporated under reduced pressure to afford the target product 1-BOC-3-hydroxymethylpiperazine (2.71 g, 99.6% yield) as a solid. The structure of the product was confirmed by 1H-NMR (CDCl3): δ 1.46 (9H, s), 2.12 (1H, br s), 2.64-3.01 (6H, br s), 3.47-3.53 (1H, m), 3.62-3.67 (1H, m), 3.89 (2H, br s).
