抗癌吲哚生物碱TMC-205的合成研究
Synthesis Study of Anticancer Indole Alkaloid TMC-205
孙维浩 1李涛 1王雪琴 1江世智 1雷婷1
作者信息
- 1. 大理大学药学院,云南大理 671000;云南省滇西抗病原植物资源筛选研究重点实验室,云南大理 671000
- 折叠
摘要
目的 以经济、简洁、高效的Pinnick氧化反应合成具有抗癌活性的吲哚生物碱TMC-205.方法 使用6-溴吲哚-3-甲醛作为起始原料,经过Heck-dehydration反应制备底物2.随后,以Pinnick氧化反应最优条件合成吲哚生物碱TMC-205.结果 完成了 Pinnick氧化反应的最优条件探索,并以78％的产率合成了 TMC-205.结论 本文提出了一种Pinnick氧化合成TMC-205的最佳方案,为TMC-205及其类似物的深入研究和合成提供了有力的支撑.
Abstract
Objective Employ the economically,concisely,and efficiently executed Pinnick oxidation reaction for the synthesis of the indole alkaloid TMC-205,which exhibited the anticancer activity.Methods Starting with 6-bromoindole-3-formaldehyde as the initial material,substrate 2 was prepared through a Heck-dehydration reaction.Subsequently,under the optimized conditions of the Pinnick oxidation reaction,the indole alkaloid TMC-205 was synthesized.Results The optimal conditions for the Pinnick oxidation reaction have been successfully identified,resulting in the synthesis of TMC-205 with a yield of 78％.Conclusion This paper proposes an optimal strategy for the Pinnick oxidation synthesis of TMC-205,providing robust support for the in-depth investigation and synthesis of TMC-205 and its analogs.
关键词
TMC-205/抗癌/吲哚生物碱/Heck-dehydration反应/Pinnick氧化Key words
TMC-205/anticancer/indole alkaloid/Heck-dehydration reaction/Pinnick oxidation引用本文复制引用
基金项目
国家自然科学基金项目(22361002)
云南省地方本科高校基础研究联合专项-面上项目(202101A0070315)
云南省科技厅基础研究专项-面上项目(202201AT070175)
出版年
2024
NETL
NSTL
万方数据