Journal
MOLECULES
Volume 25, Issue 5, Pages -Publisher
MDPI
DOI: 10.3390/molecules25051233
Keywords
palladium; indole; indomethacin; C-H functionalization
Funding
- program for Guangdong Introducing Innovative and Entrepreneurial Teams [2017ZT07C069]
- National Natural Science Foundation of China [21801260, 21971267]
- 1000-Youth Talents Plan
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We developed an efficient method for synthesis of substituted N-benzoylindole via Pd(II)-catalyzed C-H functionalization of substituted N-(2-allylphenyl)benzamide. The reaction showed a broad substrate scope (including N-acetyl and N-Ts substrates) and substituted indoles were obtained in good to excellent yields. The most distinctive feature of this method lies in the high selectivity for N-benzoylindole over benzoxazine, and this is the first example of Pd(II)-catalyzed synthesis of substituted N-benzoylindole. Notably, this new method was applied for the synthesis of key intermediate of indomethacin.
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