A Novel and Enantioselective Total Synthesis of (20S)-Camptothecin via a Sharpless Asymmetric Dihydroxylation Strategy

作者：Zhao Lei; Xiong Fang Jun; Chen Wen Xue; Chen Fen Er^*

来源：Synthesis, 2011, (24): 4045-4049.

DOI：10.1055/s-0031-1289575

• total synthesis
• stereoselectivity
• asymmetric catalysis
• antitumor agents
• Heck reaction

A novel and efficient asymmetric total synthesis of (20S)-camptothecin has been accomplished in an overall yield of 12% starting from the commercially available 2-methoxynicotinic acid. The key step in the sequence is the Sharpless asymmetric dihydroxylation of a 4-(but-1-en-2-yl) pyridine derivative to establish the stereocenter of (20S)-camptothecin.

• 出版日期2011-12
• 单位复旦大学