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Chapter One – Larock Reaction in the synthesis of heterocyclic compounds
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The indole ring is one of the most common features in natural products and small molecules with important bioactivity. Larock reported a new methodology for the synthesis of the indole ring system based on the palladium-catalyzed heteroannulation of 2-iodoaniline and substituted alkyne moieties. This procedure was subsequently extended to the preparation of other nitrogen- and oxygen- containing heterocycles. This is the process of choice for the synthesis of a large number of heterocyclic derivatives, as it provides outstanding regioselectivity and good to excellent yields.
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HERRAIZ COBO, Jesús, ALBERICIO PALOMERA, Fernando and ÁLVAREZ DOMINGO, Mercedes. Chapter One – Larock Reaction in the synthesis of heterocyclic compounds. Advances in Heterocyclic Chemistry. 2015. Vol. 116, num. 1-35. ISSN 0065-2725. [consulted: 25 of May of 2026]. Available at: https://hdl.handle.net/2445/65732