期刊
JOURNAL OF ORGANIC CHEMISTRY
卷 80, 期 1, 页码 471-481出版社
AMER CHEMICAL SOC
DOI: 10.1021/jo502463d
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资金
- Lundbeck Foundation
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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