2-Carboxyindole moiety was an important heterocyclic system in the nature products as well as a number of synthetic drugs. This type of compounds attracted more attention because of their various potential bioactivities such as antifungal, antibacterial, cytotoxic, and neuroregulation (Fig. 1). 1 More than ten efficient synthetic methods approaching indole-2-carboxylic acid ester have been reported 2 using metal-catalyzed coupling approaches and the azides ...