Journal
JOURNAL OF ORGANIC CHEMISTRY
Volume 80, Issue 1, Pages 471-481Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jo502463d
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Funding
- Lundbeck Foundation
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Privileged structures such as 2-arylindoles are recurrent molecular scaffolds in bioactive molecules. We here present an operationally simple, high yielding and scalable method for regioselective 3-acylation of 2-substituted indoles under basic conditions using functionalized acid chlorides. The method shows good tolerance to both electron-withdrawing and donating substituents on the indole scaffold and gives ready access to a variety of functionalized 3-acylindole building blocks suited for further derivatization.
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