摘要
Three pairs of novel 2-aryl-3,4,5-trihydroxypiperidines （6-8 and their enantiomers）, the piperidine analogues of the pyrrolidine alkaloids radicamine A and radicamine B, were prepared from six- membered cyclic nitrones through a concise two-step procedure, i.e., Grignard reagent addition and deprotection. These novel polyhydroxylated piperidine iminosugars were assayed against 10 types of enzymes. Only compound 8 exhibited weak inhibition （IC50 1080 μmol/L） against β-galactosidase from rat intestinal lactases.
Three pairs of novel 2-aryl-3,4,5-trihydroxypiperidines （6-8 and their enantiomers）, the piperidine analogues of the pyrrolidine alkaloids radicamine A and radicamine B, were prepared from six- membered cyclic nitrones through a concise two-step procedure, i.e., Grignard reagent addition and deprotection. These novel polyhydroxylated piperidine iminosugars were assayed against 10 types of enzymes. Only compound 8 exhibited weak inhibition （IC50 1080 μmol/L） against β-galactosidase from rat intestinal lactases.
基金
Financial support from National Basic Research Program of China (Nos. 2012CB822101 and 2011CB808603)
the Natural Science Foundation of China (Nos. 21272240 and 21102149)
