Ac2O/K2CO3/DMSO: an efficient and practical reagent system for the synthesis of nitriles from aldoximes |
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Authors: | Yaoping Song Dongguo Shen Qinghua Zhang Bo Chen Guangyu Xu |
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Affiliation: | 1. Key Laboratory of Chemical Biology and Traditional Chinese Medicine Research (Ministry of Education), College of Chemistry and Chemical Engineering, Hunan Normal University, Changsha 410081, China;2. Research and Development, Hunan Fangsheng Pharmaceuticals Limited, Changsha 410205, China |
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Abstract: | The transformation of aldoximes to nitriles using acetic anhydride as dehydration agent under mild reaction conditions is reported. The reaction, which proceeds under weak alkaline condition, allows for the conversion of a range of aldoximes including aromatic aldoximes, alphatic aldoximes, and heterocyclic aldoximes in good to excellent yields. This method has also been successfully applied to the synthesis of calcium channel blocker nilvadipine in pilot scale. |
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Keywords: | Dehydration Aldoximes Nitriles Acetic anhydride Synthesis Nilvadipine |
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