New synthetic strategy for preparation of the anticoagulant drug Rivaroxaban via an asymmetric Henry reaction |
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Authors: | Pavel Drabina Viola Feixová Miloš Sedlák |
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Affiliation: | Institute of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, Studentská 573, 532 10 Pardubice, Czech Republic |
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Abstract: | A new synthetic approach towards the anticoagulant drug (S)-Rivaroxaban was described. This reaction sequence involved six steps overall, starting from commercially available and inexpensive N-(4-aminophenyl)morpholin-3-one. The stereogenic centre was introduced by an asymmetric Henry reaction catalysed by the complex of copper(II) acetate and (2R,5S)-2-(pyridine-2-yl)imidazolidine-4-one with 87% ee. The individual reaction steps proceeded with high yields and did not require any unusual or expensive reagents. |
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Keywords: | Rivaroxaban Anticoagulant drug Henry reaction Enantioselective catalysis |
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