抗癌吲哚生物碱TMC-205的合成研究  

Synthesis Study of Anticancer Indole Alkaloid TMC-205

作　　者：孙维浩 李涛 王雪琴 江世智 雷婷 SUN Weihao;LI Tao;WANG Xueqin;JIANG Shizhi;LEI Ting(School of Pharmacy,Dali University,Dali 671000,China;Yunnan Key Laboratory of Screening andResearch on Anti-pathogenic Plant Resources from West Yunnan,Dali 671000,China)

机构地区：[1]大理大学药学院,云南大理671000 [2]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

出　　处：《云南中医药大学学报》2024年第4期54-60,共7页Journal of Yunnan University of Chinese Medicine

基　　金：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(202101AO070315);云南省科技厅基础研究专项-面上项目(202201AT070175)。

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。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 

分 类 号：R284.3[医药卫生—中药学]