Synlett 2007(2): 0211-0214  
DOI: 10.1055/s-2007-967998
LETTER
© Georg Thieme Verlag Stuttgart · New York

Practical Regioselective Bromination of Azaindoles and Diazaindoles

Fabrice Gallou*a,, Jonathan T. Reevesa, Zhulin Tana, Jinhua J. Songa, Nathan K. Yeea, Christian Harckenb, Pingrong Liub, David Thomsonb, Chris H. Senanayakea
a Department of Chemical Development, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Rd, P.O. Box 368, Ridgefield, CT 06877-0368, USA
Fax: +41(61)6962711; e-Mail: fabrice.gallou@novartis.com;
b Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Rd, P.O. Box 368, Ridgefield, CT 06877-0368, USA
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Publikationsverlauf

Received 31 October 2006
Publikationsdatum:
24. Januar 2007 (online)

Abstract

A mild and efficient synthesis of various 3-brominated azaindoles and diazaindoles was developed by regioselective halogenation of the parent systems. This practical and high-yielding transformation was achieved with copper(II) bromide in acetonitrile at room temperature.

1

Current address: Novartis Pharma AG, Chemical and Analytical Development, Werk Klybeck, Postfach, 4002 Basel, Switzerland. This address should be used for correspondence.