Department of Medicinal Chemistry, Helmholtz Centre for Infection Research, Braunschweig, Germany.
Angew Chem Int Ed Engl. 2012 Apr 2;51(14):3401-4. doi: 10.1002/anie.201108749. Epub 2012 Feb 29.
Keep me skipped: a highly convergent total synthesis of ripostatin B, an inhibitor of the bacterial RNA polymerase, is described. The key steps to construct and avoid isomerization of the skipped triene are a double Stille cross-coupling reaction and a ring-closing metathesis. Furthermore, 15-deoxyripostatin A, a stable and conformationally locked analogue of ripostatin A, was prepared and tested in vivo.
本文描述了细菌 RNA 聚合酶抑制剂里波他汀 B 的高度会聚全合成。构建和避免跳过三烯异构化的关键步骤是双 Stille 交叉偶联反应和环 closing metathesis。此外，还制备并测试了 15-脱氧里波他汀 A，它是里波他汀 A 的稳定和构象锁定类似物。
