Chinese Journal of Organic Chemistry    

吲哚生物碱Catharanthine合成研究进展

王雪倩a,b, 段宝忠*,b, 田红畅*,a, 张磊*,a   

  1. a海军军医大学药学院/教育部真菌感染性疾病医药基础研究创新中心 上海 200433;
    b大理大学药学院 大理 671000
  • 收稿日期:2025-09-22 修回日期:2025-10-24
  • 基金资助:
    国家自然科学基金(82504962、82225047、82170274)、教育部真菌感染性疾病医药基础研究创新中心开放课题(YXX2024-KF02-02)、国家重点研发计划(2024YFC3506500、2024YFC3506400)、浙江省自然科学基金(LZ24H280003)

Research Progress in Synthesis of Indole Alkaloid Catharanthine

Wang Xueqiana,b, DuanBaozhong*,b, Tian Hongchang*,a, Zhang Lei*,a   

  1. aDepartment of Pharmaceutical Botany, School of Pharmacy, Naval Medical University/ The Center for Basic Research and Innovation of Medicine and Pharmacy (MOE), Shanghai 200433;
    bCollege of Pharmaceutical Science, Dali University, Dali 671000
  • Received:2025-09-22 Revised:2025-10-24
  • Contact: *E-mail: leizhang100@163.com; TianHC8023@163.com; bzduan@126.com.
  • Supported by:
    The National Natural Science Foundation of China (No.82504962, 82225047, 82170274), Open Research Project of the Ministry of Education Innovation Center for Basic Medical Research on Fungal Infectious Diseases (No. YXX2024-KF02-02), National Key Research and Development Program of China (No. 2024YFC3506500, 2024YFC3506400), and Zhejiang Provincial Natural Science Foundation of China (No. LZ24H280003).

Catharanthine, an iboga-type indole alkaloid isolated from Catharanthus roseus, features a pentacyclic framework with three stereocenters. As a key structural fragment of the anticancer drugs vinblastine and its analogue vincristine, its complex and unique chemical architecture has made it a hotspot in synthetic studies. In recent years, its complete biosynthetic pathway has been elucidated and functionally reconstructed in heterologous systems such as yeast and Nicotiana benthamiana. Since 1969, 18 research groups have reported chemical syntheses of catharanthine, encompassing racemic, asymmetric, and biomimetic syntheses, as well as various transition-metal-catalyzed approaches. This review chronologically summarizes the advances in both the biosynthesis and chemical synthesis of catharanthine and offers perspectives on future research directions.

Key words: Catharanthine, indole alkaloid, biosynthesis, total synthesis