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Benzoic Acid: an Efficient and Rapid Catalyst for the Synthesis of α-Hydroxyl(indolyl)ethanones from Indoles |
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| Authors: | L&# Guanghui CHENG Xu ZHENG Yang LI Weijian HAI Li WU Yong |
| Affiliation: | Key Laboratory of Drug-targeting, Ministry of Education, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041, P. R. China |
| Abstract: | An efficient method for regioselective Friedel-Crafts alkylations of indole using arylglyoxals in the presence of benzoic acid has been discovered. The reactions proceeded smoothly at room temperature under metalfree conditions and generated the corresponding products in good to excellent yields. This methodology has a broad substrate scope and opens up an interesting and attractive avenue for the synthesis of α-hydroxyl(indolyl)-ethanones. |
| Keywords: | Friedel-Crafts alkylation Indole Arylglyoxal Benzoic acid |
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