Department of Chemistry, The Scripps Research Institute, La Jolla, California 92037, United States.
J Am Chem Soc. 2012 May 23;134(20):8432-5. doi: 10.1021/ja303937y. Epub 2012 May 14.
A scalable, divergent synthesis of bioactive meroterpenoids has been developed. A key component of this work is the invention of "borono-sclareolide", a terpenyl radical precursor that enables gram-scale preparation of (+)-chromazonarol. Subsequent synthetic operations on this key intermediate permit rapid access to a variety of related meroterpenoids, many of which possess important biological activity.
一种可扩展的、多样化的生物活性倍半萜类化合物的合成方法已经被开发出来。这项工作的一个关键组成部分是“硼代喇叭茶内酯”的发明,这是一种萜烯基自由基前体,可以实现(+)-变色醇的克级制备。对这个关键中间体的后续合成操作可以快速获得多种相关的倍半萜类化合物,其中许多具有重要的生物活性。