Synthesis and Bioactivity of Isosteviol Derivatives: A Facile Method for Preparation of Ent-16α-hydroxy-15β-hydroxymethylbeyeran-19-oic Acid  

作　　者：Jing Chao TAO Guo Qiang TIAN Yan Bing ZHANG Yu Qin FU Gui Fu DAI Ya WU 

机构地区：[1]Department of Chemistry, Zhengzhou University, Zhengzhou 450052

出　　处：《Chinese Chemical Letters》2005年第11期1441-1444,共4页中国化学快报（英文版）

基　　金：the National Natural Science Foundation of China(20372059);Natural Science Foundation of Henan Province for the financial support(0311020500).

摘　　要：In this paper, two new compounds, ent-16α-hydroxy-15β-hydroxymethylbeyeran-19-oic acid 4 and its ethyl ester 5 were synthesized in good yield with a facile method that has never been reported. The mechanism of this reaction was discussed and the mono-hydroxymethylation of carbonyl compound with two α-hydrogens via Tollens＇ reaction was firstly achieved. Compounds 2-5 were tested for activity of inhibition against glycosidases, among which 5 displays good inhibition of β-glucosidase and α-mannase, respectively.In this paper, two new compounds, ent-16α-hydroxy-15β-hydroxymethylbeyeran-19-oic acid 4 and its ethyl ester 5 were synthesized in good yield with a facile method that has never been reported. The mechanism of this reaction was discussed and the mono-hydroxymethylation of carbonyl compound with two α-hydrogens via Tollens＇ reaction was firstly achieved. Compounds 2-5 were tested for activity of inhibition against glycosidases, among which 5 displays good inhibition of β-glucosidase and α-mannase, respectively.

关 键 词：ISOSTEVIOL 1 3-diol hydroxylation. 

分 类 号：O623.413[理学—有机化学]