Department of Chemistry and Biochemistry, University of Calfornia, San Diego, 9500 Gilman Drive, La Jolla, California 92093-0358, USA.
Org Lett. 2012 Nov 2;14(21):5396-9. doi: 10.1021/ol3023006. Epub 2012 Oct 16.
The total synthesis of FD-895 was completed through a strategy that featured the use of a tandem esterification ring-closing metathesis (RCM) process to construct the 12-membered macrolide and a modified Stille coupling to append the side chain. These studies combined with detailed analysis of all four possible C16-C17 stereoisomers were used to confirm the structure of FD-895 and identify an analog with an enhanced subnanomolar bioactivity.
FD-895 的全合成是通过一种策略完成的，该策略的特点是使用串联酯化环 closing 复分解（RCM）过程构建 12 元大环内酯和修饰的 Stille 偶联来附加侧链。这些研究结合对所有四个可能的 C16-C17 立体异构体的详细分析，用于确认 FD-895 的结构并鉴定出具有增强的亚纳摩尔生物活性的类似物。
