A unified approach to polyene macrolides: Synthesis of candidin and nystatin polyols
A unified approach to polyene macrolides: Synthesis of candidin and nystatin polyols
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DOI：
10.1073/pnas.0401552101
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发表时间：
2004-08-17
影响因子：
11.1
通讯作者：
Rychnovsky, SD
中科院分区：
文献类型：
--
作者：
Kadota, I;Hu, YQ;Rychnovsky, SD
多烯大环内酯类抗生素是天然存在的抗真菌剂。这类药物包括已广泛用于治疗全身真菌感染的阿替霉素B。已经设计了一种通用的合成策略来制备与多烯大环内酯相关的多元醇链。氰醇丙酮化物烷基化被用来组装碳骨架，和一个简单的修改策略允许先进的中间体被转化为念珠菌素多元醇或制霉菌素多元醇。将念珠菌素多元醇进一步加工成受保护的念珠菌素糖苷配基。这一策略将适用于其他多烯大环内酯类天然产物。
Polyene macrolide antibiotics are naturally occurring antifungal agents. Members of this class include amphotericin B, which has been used widely to treat systemic fungal infections. A general synthetic strategy has been devised to prepare polyol chains associated with the polyene macrolides. Cyanohydrin acetonide alkylations were used to assemble the carbon skeleton, and a simple modification of the strategy allowed an advanced intermediate to be converted to either the candidin polyol or the nystatin polyol. The candidin polyol was further elaborated to a protected candidin aglycone. This strategy will be applicable to other members of the polyene macrolide natural products.