Several synthetic methods have been developed for the synthesis of indoloquinolines (2) because this core structure has been well established as potent antibacterial, antifungal, antimicrobial, anti-HIV, anticancer and antimalarial agents. In response to the importance of indoloquinolines (2), the development of novel and innovative synthetic methodologies is still an active area of research for organic chemists in order to increase the accessibility to diverse derivatives of this important core scaffold which is very useful for drug discovery. In this work, we reported the conceptually expedient method to prepare indoloquinolines (2) using the N2-extrusion of simple ortho-alkynylarylketone (1). This transformation employed domino reactions in one synthetic operation which is a challenging task to concisely furnish the target product 2 in moderate to good yields.

Synthesis of indoloquinolines via domino reactions of ortho-alkynylarylketones

256th National Meeting (2018)

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