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Synthesis of Pyrido[1,2-a]indole Malonates and Amines through Aryne Annulation

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journal contribution
posted on 16.03.2012, 00:00 by Donald C. Rogness, Nataliya A. Markina, Jesse P. Waldo, Richard C. Larock
Pyrido­[1,2-a]­indoles are known as medicinally and pharmaceutically important compounds, but there is a lack of efficient methods for their synthesis. We report a convenient and efficient route to these privileged structures starting from easily accessible 2-substituted pyridines and aryne precursors. A small library of compounds has been synthesized utilizing the developed method, affording variously substituted pyrido­[1,2-a]­indoles in moderate to good yields.