Abstract: A series of piperidine derivatives was synthesized using 1,5-diols as starting materials. The procedures include the sulfonylation of 1,5-diols to active 1,5-disulfonates followed by the cyclization of the 1,5-disulfonates with primary amines. The effects of reaction temperature, time on the annulation were further explored. It was disclosed that when the solvent was primary amine, reaction temperature was 90~100 ℃, and reaction time was 18 h, the yields of 74%~94% for annulations could be reached.

Key words: diols, piperidine, iminosugar, Organic Synthesis