Efficient synthesis of morolic acid and related triterpenes starting from betulin

被引：33

作者：

Zhang, Pu ^{[1
]}

Hao, Jia ^{[1
]}

Liu, Jun ^{[2
]}

Zhang, Luyong ^{[2
]}

Sun, Hongbin ^{[1
]}

机构：

[1] China Pharmaceut Univ, Coll Pharm, Ctr Drug Discovery, Nanjing 210009, Peoples R China

[2] China Pharmaceut Univ, Jiangsu Ctr Drug Screening, Nanjing 210038, Peoples R China

来源：

TETRAHEDRON | 2009年 / 65卷 / 22期

关键词：

ANTI-AIDS AGENTS; MORONIC ACID; GLYCOGEN-PHOSPHORYLASE; IN-VITRO; CONSTITUENTS; DERIVATIVES; MATURATION; INHIBITOR; ACCESS; STEP;

D O I：

10.1016/j.tet.2009.03.100

中图分类号：

O62 [有机化学];

学科分类号：

070303 [有机化学];

摘要：

Morolic acid (1) is a naturally occurring pentacyclic triterpene whose derivatives exhibit promising anti-HIV and other biological activities. An efficient synthesis of I has been accomplished in 11 steps with a total yield of 24% starting from betulin. Some related natural triterpenes including moradiol (4), acridocarpusic acid D (5), acridocarpusic acid E (6), and moronic aldehyde (7) have also been synthesized. Biological assay results showed that 1, 5, and 6 exhibited moderate inhibitory activity against glycogen phosphorylase. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：4304 / 4309

页数：6

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