Aminohaloborane in Organic Synthesis. Simple Synthesis of Indoles and 1-Acyl-3-Indolinones Using Specific Ortho α-Chloroacetylation of Anilines
T. Sugsawa, M. Adachi, K. Sasakura, A.Kitagawa, J. Org. Chem., Vol. 44, No. 4, 1979
The search for an efficient synthesis of indoles has been a problem for nearly a century in organic synthesis. Beginning with the classical Fisher and Reissert methods, many reports have appeared from practical and/or academic points of view. Among these, only the Leimgruber method is a general one for synthesizing indoles which are substituted in the benzene ring but not in the heterocyclic nucleus.
We present here a new, efficient method for synthesizing such substituted indoles in two steps from anilines.
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