Synthesis Study of Anticancer Indole Alkaloid TMC-205
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.
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