Palladium-catalyzed carbonylation of haloindoles: no need for protecting groups.
[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.
Kumar
Kamal
K
Leibniz-Institut für Organische Katalyse an der Universität Rostock e.V. (IfOK), Buchbinderstrasse 5-6, D-18055 Rostock, Germany.
Zapf
Alexander
A
Michalik
Dirk
D
Tillack
Annegret
A
Heinrich
Timo
T
Böttcher
Henning
H
Arlt
Michael
M
Beller
Matthias
M