An effective and facile method for the synthesis of N-alkylated hydroxylpyrrolidine and hydroxylpiper- idine is described, A number of N-alkyl substituted iminosugars were prepared using iodine-induced intramolecular ...An effective and facile method for the synthesis of N-alkylated hydroxylpyrrolidine and hydroxylpiper- idine is described, A number of N-alkyl substituted iminosugars were prepared using iodine-induced intramolecular cyclization of acyclic alkenylamines as key step.展开更多
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 nitro...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.展开更多
基金supported by the Project of Discovery, Evaluation and Transformation of Active Natural Compounds, Strategic Biological Resources Service Network Programme of Chinese Academy of Sciences(No. ZSTH-006)the National Natural Science Foundation of China(Nos. 21372215 and 21772192)Chinese Academy of Sciences(No.KFJ-SW-STS-143-1)
文摘An effective and facile method for the synthesis of N-alkylated hydroxylpyrrolidine and hydroxylpiper- idine is described, A number of N-alkyl substituted iminosugars were prepared using iodine-induced intramolecular cyclization of acyclic alkenylamines as key step.
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)
文摘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.
