Stereoselective transformation of pyrazinones into substituted analogues of cis-5-amino-6-oxo-2-piperidinemethanol and cis-5-amino-2-piperidinemethanol |
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| Authors: | Joeri RogiersWim M De Borggraeve Suzanne M ToppetFrans Compernolle Georges J Hoornaert |
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| Institution: | Department of Organic Chemistry, Laboratorium voor Organische Synthese, K.U.Leuven, Celestijnenlaan 200F, B-3001 Leuven, Belgium |
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| Abstract: | Various analogues of cis-5-amino-6-oxo-2-piperidinemethanol and cis-5-amino-2-piperidinemethanol have been prepared via Diels-Alder reaction of substituted pyrazinones with ethene followed by acid methanolysis of the bridged lactam adducts. Further reduction of the resulting methyl 2-piperidinecarboxylate ester compounds led to the corresponding 2-piperidinemethanol products that were converted into potential SP antagonists. |
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| Keywords: | substituted piperidines substituted piperidinones Diels-Alder reaction Substance P antagonists |
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