Department of Chemistry, University of Oxford, Chemistry Research Laboratory, Mansfield Road, Oxford, OX1 3TA, UK.
Chemistry. 2018 May 7;24(26):6747-6754. doi: 10.1002/chem.201800046. Epub 2018 Mar 9.
Salinosporamide A is a β-lactone proteasome inhibitor currently in clinical trials for the treatment of multiple-myeloma. Herein we report a short synthesis of this small, highly functionalized, biologically important natural product that uses an oxidative radical cyclization as a key step and allows for the preparation of gram quantities of advanced synthetic intermediates.
沙利度胺 A 是一种β-内酰胺蛋白酶体抑制剂，目前正在进行多发性骨髓瘤的临床试验。在此，我们报道了这种小型、高度功能化、具有生物学重要性的天然产物的简短合成方法，该方法使用氧化自由基环化作为关键步骤，并允许制备克级别的高级合成中间体。
