Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 10, Issue 43, Pages 8605-8608Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c2ob26604k
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Funding
- National Natural Science Foundation of China [21202138]
- Xiangtan University [11QDZ20]
- Hunan Provincial Natural Science Foundation of China [12JJ7002]
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A practical Bronsted acid promoted benzylic C-H functionalization of 2-methylazaarenes and nucleophilic addition to aldehydes was developed in good to excellent yields. A six-membered hydrogen-bonding transition state is proposed to be crucial for the reaction. Ready availability of the two starting materials, the use of acetic acid as the catalyst and the facile reaction conditions will guarantee this synthetic method attractive to the synthesis of bioactive pyridine and quinoline derivatives.
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