Efficient Synthesis of Natural Products Having Intriguing Biological Activities Useful for Drug Discovery

我们研究了具有有趣的生物活性的天然产物的全合成，对药物发现有用。因此，我们开发了高效的方法来合成dyshiherbine（谷氨酸受体激动剂）、phoactomycin B和fostriecin、PP2A抑制剂和neooxazolomycin（抗肿瘤抗生素）。此外，我们开发了一种依赖于In（III）催化的Conia-ene反应构建杂环的新方法，并实现了蛋白酶体抑制剂salinosporamide a的全合成。

We have studied on the total synthesis of natural products having intriguing biological activities useful for drug discovery. As a result, we have developed efficient methodologies for the synthesis of dyshiherbaine, a glutamate receptor agonist, phoslactomycin B and fostriecin, PP2A inhibitors, and neooxazolomycin, an antitumor antibiotic. In addition, we have developed a new methodology for the construction of heterocycles which relies on an In(III)-catalyzed Conia-ene reaction, and achieved the total synthesis of salinosporamide A, a proteasome inhibitor.