Transition-metal-free synthesis of (Z)-3-ylidenephthalides from 2-acyl-benzoic acids |
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Authors: | Xinhua He Fengtian Xue |
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Institution: | Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 Penn Street, Baltimore, MD 21201, United States |
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Abstract: | We report a highly efficient method for the synthesis of (Z)-3-ylidenephthalides via intramolecular cyclization of readily available 2-acyl-benzoic acids mediated by TSTU at room temperature. Using this method, diversely substituted (Z)-3-ylidenephthalides have been generated in good to excellent yields. The application of the method is highlighted by gram-scale preparation of the antiplatelet drug n-butylphthalide. |
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Keywords: | (Z)-3-Ylidenephthalides 2-Acyl-benzoic acid Intramolecular cyclization Enol n-Butylphthalide |
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