School of Chemistry, The University of Sydney, NSW 2006, Australia.
Org Lett. 2010 Dec 3;12(23):5576-9. doi: 10.1021/ol1024663. Epub 2010 Nov 4.
The first total synthesis of symplostatin 4, a marine cyanobacterium-derived natural product, is described. Notable features of the route include the efficient preparation of three key fragments and final assembly to the natural product via sequential imide and amide couplings. Symplostatin 4 was also demonstrated to possess significant antimalarial activity (ED(50) of 74 nM against Plasmodium falciparum, strain 3D7).
本文描述了海洋蓝细菌来源的天然产物 symplostatin 4 的首次全合成。该路线的显著特点包括通过连续的酰亚胺和酰胺偶联，有效地制备了三个关键片段，并最终对天然产物进行了组装。此外，symplostatin 4 还表现出显著的抗疟活性（对 Plasmodium falciparum 株 3D7 的 ED50 为 74 nM）。
