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 

作者机构：Department of Chemistry Zhengzhou University Zhengzhou 450052 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2005年第16卷第11期

页      面：1441-1444页

核心收录：

学科分类：081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0703[理学-化学] 

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

主　　题：Isosteviol 1,3-diol hydroxylation. 

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.