Acetic Acid → HCID 46785855, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of piperazine-1-carboxylic acid tert-butyl ester (1.5 g, 8.05 mmol) stirring in anhydrous THF (20 mL) and water (0.2 mL) was added glacial acetic acid (1.45 mL, 24.2 mmol), followed by sodium cyanoborohydride (758 mg, 12.1 mmol). The reaction mixture was stirred at 60° C. for 12 h, quenched with 10% aqueous NaHCO3 (50 mL), extracted with EtOAc and dried (MgSO4) to give a colourless oil which was purified by silica chromatography to give 4-(tetrahydro-pyran-4-yl)-piperazine-1-carboxylic acid tert-butyl ester (0.54 g, 25%), as a white solid. BOC-deprotection was carried out as in Reference Example 3 to give the title compound (0.30 g, 88%).

Provenance & Evidence