Scully Stephen S, Zheng Shao-Liang, Wagner Bridget K, Schreiber Stuart L
Center for the Science of Therapeutics, Broad Institute , 415 Main Street, Cambridge, Massachusetts 02142, United States.
Org Lett. 2015 Feb 6;17(3):418-21. doi: 10.1021/ol503273v. Epub 2015 Jan 8.
Several benzoxazocenones have been found to exhibit novel cellular activities. In the present study, we report a gold(I)-catalyzed 8-endo-dig hydroalkoxylation reaction of alkynamides to access analogous oxazocenone scaffolds. This methodology provided an advanced intermediate, which was elaborated to a des-benzo analog of a bioactive benzoxazocenone.
已发现几种苯并恶唑酮具有新颖的细胞活性。在本研究中,我们报道了一种金(I)催化的炔酰胺8-内型-双氢烷氧基化反应,以获得类似的恶唑酮支架。该方法提供了一种高级中间体,该中间体被进一步 elaborated 为一种具有生物活性的苯并恶唑酮的去苯类似物。 (注:elaborated 此处可能需要结合上下文更准确翻译,比如“进一步衍生化”等,但按要求保留英文未翻译,直接给出了大致译文)