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Letters in Organic Chemistry

Editor-in-Chief

ISSN (Print): 1570-1786
ISSN (Online): 1875-6255

Regioselective Amination of 3-Bromoindolylmaleimide with Amines

Author(s): Di-Fa Jiang, Yan-Wu Yang, Zhi-Yu Shao and Sheng-Yin Zhao

Volume 7 , Issue 2 , 2010

Page: [144 - 148] Pages: 5

DOI: 10.2174/157017810790796200

Price: $65

Abstract

3-Bromoindolylmaleimide and bisindolylmaleimide were synthesized from succinimide in three steps sequnence consisting of bromination, N-methylation and indole addition in the presence of magnesium and bromoethane. They were subjeced to the regioselective amination with substituted amines to provide 3-aminoindolylmaleimides, 3- amino-N-alkylated indolylmaleimides and N-alkylated bisindolylmaleimides in good yields. The resulting indolylmaleimides represent a new class of potentially bioactive compounds.

Keywords: 3-Bromoindolylmaleimide, bisindolylmaleimide, regioselective amination, reaction mechanism


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