Synthesis of benzo-annulated 1,3-oxazine derivatives through the multi-component reaction of arynes with N-heteroaromatics and aldehydes or ketones |
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| Authors: | Peng Liu Min Lei Lihong Hu |
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| Institution: | 1. Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China;2. Shanghai Research Center for Modernization of Traditional Chinese Medicine, Shanghai Institute of Materia Medica, Shanghai 201203, China |
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| Abstract: | A multi-component reaction involving arynes, N-heteroaromatic compounds (including pyridine, quinoline, and isoquinoline), and aldehydes or ketones for the synthesis of benzo-annulated 1,3-oxazine derivatives has been described. The whole process is carried out under mild conditions and furnishes the desired products in 35–85% yields. Furthermore, regioselectivity and diastereoselectivity can be observed when using 3-OMe aryne precursor in this reaction. |
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| Keywords: | Aryne N-Heteroaromatic compound 1 3-Oxazine Multi-component reactions Cyclization |
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