Ghosh Arun K, Xi Kai
Department of Chemistry, Purdue University, 560 Oval Drive, West Lafayette, IN 47907, USA.
Angew Chem Int Ed Engl. 2009;48(29):5372-5. doi: 10.1002/anie.200902338.
Quick access: A concise and efficient formal synthesis of platencin has been accomplished in nine steps from a commercially available starting material. The synthesis utilized only one protecting group. The base-catalyzed Michael cyclization of precursor 1 afforded the key diketone 2, which was converted into the desired core structure 4 via the radical intermediate 3.
从市售起始原料出发,经九步反应简洁高效地完成了普拉替尼的形式合成。该合成仅使用了一个保护基。前体1的碱催化迈克尔环化反应得到关键二酮2,其通过自由基中间体3转化为所需的核心结构4。