Abstract:Objective Employing the economically, concisely, and efficiently executed Pinnick oxidation reaction for the synthesis of the indole alkaloid TMC-205, which exhibits anticancer activity. Methods Using compound 2 as the starting material, we aim to determine the optimal process for synthesizing the indole alkaloid TMC-205 by optimizing the conditions of the Pinnick oxidation reaction. 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.