Journal
ACS COMBINATORIAL SCIENCE
Volume 20, Issue 10, Pages 573-578Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acscombsci.8b00071
Keywords
cyclization; indole; Lewis acid; 1H-pyrazole; ring-opening
Funding
- Science and Engineering Research Board, Govt. of India [EMR/2016/005008]
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An unusual transformation of indoles to pyrazoles via an aromatic ring-opening strategy has been developed. The salient feature of this strategy involves the C2-N1 bond opening and concomitant cyclization reaction of the C2=C3 bond of the indole moiety with the tosylhydrazone, which proceeds under transition-metal and ligand free conditions. This ring-opening functionalization of indoles provides a wide scope of differently substituted pyrazoles.
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