School of Pharmacy, Kitasato University, Tokyo, Japan.
J Antibiot (Tokyo). 2011 Dec;64(12):781-7. doi: 10.1038/ja.2011.90. Epub 2011 Oct 12.
The first total synthesis of extracellular factor, "Avenolide", in Streptomyces avermitilis has been achieved using a convergent approach. The stereogenic centers in two key segments were installed using Sharpless epoxidation and dihydroxylation. This synthetic study allowed the determination of the absolute configuration of avenolide as 4S,10R, and yielded important information on its structure-activity relationship.
阿维链霉菌中细胞外因子“Avenolide”的首次全合成是采用汇聚方法实现的。两个关键片段中的手性中心是利用 Sharpless 环氧化和双羟化反应来构建的。这项合成研究确定了阿维链霉菌中 Avenolide 的绝对构型为 4S,10R，并提供了关于其结构-活性关系的重要信息。
