有效霉烯胺的化学合成进展-上海有机化学研究所.PDF

DOI: 10.6023/cjoc201605015 综述与进展 有机化学 Chinese Journal of Organic Chemistry REVIEW 有效霉烯胺的化学合成进展 计 立a,b 吴国锋b 叶伟东b 陈新志*,a (a 浙江大学化学工程与生物工程学院 杭州 310027) (b 浙江医药股份有限公司研究院 新昌 312500) 摘要 有效霉烯胺是一种由有效氧胺A 经脱氮假单胞菌降解得到的 C7N 氨基环醇类 α-糖苷酶抑制剂, 同时也是有效霉 素、阿卡波糖等伪寡糖 α-糖苷酶抑制剂的核心片段. 基于其确定的化学结构和令人感兴趣的生物活性, 自从1972 年被 首次分离后, 众多合成化学家设计并完成了各种有效霉烯胺的合成路线. 综述了过去三十多年中见于文献报道的有效 霉烯胺 23 条全合成路线. 关键词 有效霉烯胺; C7N 氨基环醇; 氨基碳糖; α-糖苷酶抑制剂; 全合成 Review of Total Synthesis of Valienamine Ji, Lia,b Wu, Guofengb Ye, Weidongb Chen, Xinzhi*,a (a College of Chemical and Biological Engineering, Zhejiang University, Hangzhou 310027) b ( Research Development Center, Zhejiang Medicine Co., Ltd, Xinchang 312500) Abstract Valienamine is an α-glucosidase inhibitor belonging to C N aminocyclitols that was isolated from the microbial 7 degradation of validoxylamine A with Pseudomonas denitrificans. Moreover, valienamine is also an essential core unit in many kinds of pseudo-oligosaccharidic α-D-glucosidase inhibitors such as validamycins and acarbose. Due to the unique structural feature and interesting biological property, since the first isolation in 1972, a great deal of effort has been devoted to the de- velopment of various approaches for the efficient synthesis