Efficient Synthesis and Stereochemical Revision of Coibamide A
Efficient Synthesis and Stereochemical Revision of Coibamide A
复制标题
考巴胺 A 的高效合成和立体化学修饰
DOI：
10.1021/jacs.5b09286
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发表时间：
2015
影响因子：
15
通讯作者：
Su Wu
中科院分区：
文献类型：
--
作者：
Yao Guiyang;Pan Zhengyin;Wu Chunlei;Wang Wei;Fang Lijing;Su Wu
Coibamide A是一种高效的抗增殖环沉积肽，最初从巴拿马海洋蓝藻中分离出来。在此，我们报告了一种高效的固相策略，用于组装高度n -甲基化的环沉积肽，这对于生成coibamide A衍生物用于结构-活性关系研究是非常宝贵的。由于我们的合成研究，修正了coibamide a的两个立体化学配位，并首次实现了该天然化合物的全合成。
Coibamide A is a highly potent antiproliferative cyclodepsipeptide originally isolated from a Panamanian marine cyanobacterium. Herein we report an efficient solid-phase strategy for assembly of highlyN-methylated cyclodepsipeptides, which is invaluable in generating coibamide A derivatives for structure–activity relationship studies. As a consequence of our synthetic studies, two stereochemical assignments of coibamide A were revised and the total synthesis of this natural compound was achieved for the first time.