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Larock indole synthesis : ウィキペディア英語版 | Larock indole synthesis
The Larock indole synthesis is a heteroannulation reaction that uses palladium as a catalyst to synthesize indoles from an ortho-iodoaniline and a disubstituted alkyne. It is also known as Larock heteroannulation. The reaction is extremely versatile and can be used to produce varying types of indoles. Larock indole synthesis was first proposed by Richard C. Larock in 1991 at Iowa State University.〔Li, J.J. (2011) "Larock Indole Synthesis" in ''Name Reactions in Heterocyclic Chemistry II'', John Wiley & Sons, ISBN 978-0-470-08508-0, pp. 143–166.〕 ==Overall reaction== The reaction usually occurs with an ''o''-iodianiline or its derivatives, 2–5 equivalents of an alkyne, palladium(II) (PdII), an excess of sodium or potassium carbonate base, PPh3, and 1 equivalent of LiCl or n-Bu4NCl. N-methyl, N-acetyl, and N-tosyl derivatives of ortho-iodoanilines have been shown to be the most successful anilines that can be used to produce good to excellent yields.
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