Journal
ORGANIC LETTERS
Volume 17, Issue 1, Pages 134-137Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol503366r
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Funding
- National Natural Science Foundation of China [21032001, 21272085]
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The first C-3-dicarbonylation of indoles was realized through direct oxidative cross-coupling of indoles with methyl ketones in the presence of molecular iodine and pyrrolidine. This reaction constructed a highly efficient indolyl diketones scaffold, which might be regarded as a useful biological and pharmacological tool in the exploration of therapeutic A(2B)AR modulators. The use of inexpensive molecular iodine and pyrrolidine and a broad substrate scope make this protocol very practical. Preliminary mechanistic studies indicate that two paths are involved in this process.
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