Roethle Paul A, Chen Ingrid T, Trauner Dirk
Department of Chemistry, University of California, Berkeley, Berkeley, California 94720-1460, USA.
J Am Chem Soc. 2007 Jul 25;129(29):8960-1. doi: 10.1021/ja0733033. Epub 2007 Jun 27.
A highly convergent synthesis of archazolid B, a potent and highly selective V-ATPase inhibitor, is described. A relay ring-closing metathesis reaction was used to form the 24-membered macrocyclic lactone, whereas the sensitive cis-triene moiety of the archazolids was assembled with a modified Stille coupling.
本文描述了一种高效合成强效且高选择性V-ATP酶抑制剂阿扎唑醇B的方法。利用接力闭环复分解反应形成24元大环内酯,而阿扎唑醇类化合物中敏感的顺式三烯部分则通过改良的Stille偶联反应构建。