Palladium-Catalyzed Carbonylation of Haloindoles: No Need for Protecting Groups

Kamal Kumar, Alexander Zapf, Dirk Michalik, Annegret Tillack, Timo Heinrich, Henning Böttcher, Michael Arlt, Matthias Beller

Research output: Contribution to journalArticlepeer-review

81 Scopus citations


(Equation presented) For the first time, palladium-catalyzed carbonylations of unprotected bromoindoles have been performed successfully with different N- and 0-nucleophiles. Various indole carboxylic acid derivatives are accessible in excellent yield. For example, aminocarbonylation of 4-, 5-, 6-, or 7-bromoindole with arylethylpiperazines provides a direct one-step synthesis for CNS active amphetamine derivatives.

Original languageEnglish
Pages (from-to)7-10
Number of pages4
JournalOrganic Letters
Issue number1
StatePublished - 8 Jan 2004
Externally publishedYes


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