Reynolds Aaron J, Scott Andrew J, Turner Craig I, Sherburn Michael S
Research School of Chemistry, Australian National University, Canberra ACT 0200, Australia.
J Am Chem Soc. 2003 Oct 8;125(40):12108-9. doi: 10.1021/ja0376588.
Since 1960, only seven plant-derived anticancer drugs have received FDA approval for commercial production. Two are semisynthetic derivatives of podophyllotoxin. This paper describes concise, highly convergent, and conceptually novel approaches to (-)-podophyllotoxin and its enantiomer. These highly convergent syntheses feature a late-stage domino radical reaction to install the lactone ring and the pendant trimethoxyphenyl group.
自1960年以来，仅有七种源自植物的抗癌药物获得美国食品药品监督管理局（FDA）批准进行商业化生产。其中两种是鬼臼毒素的半合成衍生物。本文描述了一种简洁、高度汇聚且概念新颖的合成（-）-鬼臼毒素及其对映体的方法。这些高度汇聚的合成方法的特点是在后期通过多米诺自由基反应构建内酯环和悬挂的三甲氧基苯基。
