A macrocyclic approach to tetracycline natural products. Investigation of transannular alkylations and Michael additions.
A macrocyclic approach to tetracycline natural products. Investigation of transannular alkylations and Michael additions.
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DOI：
10.1021/ol302691j
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发表时间：
2012-11
期刊：
影响因子：
5.2
通讯作者：
J. Wzorek;Thomas F Knöpfel;Ioannis Sapountzis;D. A. Evans
中科院分区：
文献类型：
--
作者：
J. Wzorek;Thomas F Knöpfel;Ioannis Sapountzis;D. A. Evans
提出了一种新的四环素核心结构分析方法。关键中间体被鉴定为大环III。两个内部键（C4a-C12a和C5a-C11a）将通过连续的跨环Michael加成（III-II）和中间体II的压缩促进跨环异恶唑烷基化来构建。
A new approach to the tetracycline core structure is presented. The pivotal intermediate is identified as macrocycle III. The two interior bonds (C4a-C12a and C5a-C11a) are to be constructed through sequential transannular Michael additions (III-II) and compression-promoted transannular isoxazole alkylations from intermediate II.