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Synlett 2001; 2001(2): 0222-0225
DOI: 10.1055/s-2001-10784
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Synthesis of N-Aminoindole Ureas from Ethyl 1-Amino-6-(trifluoromethyl)-1H-indole-3-carboxylate

Michel Belley* , John Scheigetz, Pascal Dubé, Sarah Dolman
  • *Merck Frosst Centre for Therapeutic Research, Department of Medicinal Chemistry, 16711 Route Transcanadienne, Kirkland, Québec, H9H 3L1, Canada; Fax (514) 428-4900; E-mail: belley§merck.com
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Publication Date:
31 December 2001 (online)

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Two routes to the synthesis of ethyl 6-(trifluoromethyl)-1H-indole-3-carboxylate are described. N-Amination of this key intermediate with O-(diphenylphosphinyl)hydroxylamine and subsequent reactions with aryl isocyanates, using pyridine as solvent, gave the corresponding N-aminoindole ureas 1-4 in good yields.

aminations - indoles - cyclizations - urea formation - isocyanates

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