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. 2004 Jan 8;6(1):7-10.
doi: 10.1021/ol035988r.

Palladium-catalyzed carbonylation of haloindoles: no need for protecting groups

Kamal Kumar  1 , Alexander Zapf, Dirk Michalik, Annegret Tillack, Timo Heinrich, Henning Böttcher, Michael Arlt, Matthias Beller
Affiliations

Palladium-catalyzed carbonylation of haloindoles: no need for protecting groups

Kamal Kumar et al. Org Lett. .

Abstract

[reaction: see text] For the first time, palladium-catalyzed carbonylations of unprotected bromoindoles have been performed successfully with different N- and O-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.

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