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First total synthesis of papilistatin
Meng Wu1, Ling Li, An-Zheng Feng
1State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, People's Republic of China.
Organic & Biomolecular Chemistry
|February 24, 2011
Summary
Researchers achieved the first total synthesis of papilistatin, a compound with promising anticancer and antibacterial properties. This breakthrough utilized radical cyclization as a key synthetic strategy.
Area of Science:
- Organic Chemistry
- Medicinal Chemistry
- Natural Product Synthesis
Background:
- Papilistatin, a unique phenanthrene-1,10-dicarboxylic acid, has recently been isolated.
- This compound exhibits significant anticancer and antibacterial activities.
Purpose of the Study:
- To describe the first total synthesis of papilistatin.
- To establish a synthetic route for this biologically active molecule.
Main Methods:
- The synthesis employed radical cyclization as the pivotal step.
- Detailed synthetic procedures for constructing the papilistatin core structure.
Main Results:
- Successful completion of the first total synthesis of papilistatin.
- Confirmation of the compound's unique phenanthrene-1,10-dicarboxylic acid structure.
Conclusions:
- The developed synthetic route provides access to papilistatin for further biological evaluation.
- This synthesis opens avenues for exploring structure-activity relationships and developing novel therapeutic agents.
