Chem. J. Chinese Universities ›› 2020, Vol. 41 ›› Issue (10): 2137.doi: 10.7503/cjcu20200516

• Review • Previous Articles     Next Articles

Research Advances in Synthesis of Trabectedin

LI Huoming, ZHANG Fuyao()   

  1. Selection Bioscience LLC,Shanghai 201210,China
  • Received:2020-07-31 Online:2020-10-10 Published:2020-10-08
  • Contact: ZHANG Fuyao E-mail:zhangfuyao@selectionbio.com

Abstract:

As the first anti-tumor drug derived from marine natural product, trabectedin has been approved in various of countries for treatment of advanced soft tissue sarcoma and relapsed ovarian cancer. Due to its specialty and challenge in structural complexity, trabectedin has received intensive attention from both academia and industry. Total synthesis of trabectedin not only provides the platform for the academic research groups to elaborate the practicability of synthetic methodology and the art of total synthesis, but also forms the tie to connect the academia and the industry. It could establish solid basis for developing the synthetic routes of drug supply for early stage clinical trials and commercial production. From the viewpoint of structure and retrosynthetic analysis, this review focuses on the synthetic advances of trabectedin, especially on the synthetic strategies of the establishment of the rings and chiral centers therein.

Key words: Trabectedin, Lurbinetedin, Bistetrahydroisoquinoline, Generic drug, Pictet-Spengler reaction

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