Synlett

Synthesis of N-Aminoindole Ureas from Ethyl 1-Amino-6-(trifluoromethyl)-1H-indole-3-carboxylate

M Belley, J Scheigetz, P Dubé, S Dolman

Index: Belley; Scheigetz; Dube; Dolman Synlett, 2001 , # 2 p. 222 - 225

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Citation Number: 10

Abstract

Abstract: 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. Key words: aminations, indoles, cyclizations, urea formation, isocyanates