Synthesis of 4-trifluoromethylpyrido[1,2-a]pyrimidin-2-ones utilizing activated alkynoates |
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| Authors: | Geraldine CB HarrimanShannon Chi Min ZhangAndrea Crowe Robert A BennettIan Parsons |
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| Institution: | Millennium Pharmaceuticals Inc., 75 Sidney Street, Cambridge, MA 02139, USA |
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| Abstract: | The synthesis of the biologically relevant, 4-trifluoromethylpyrido1,2-a]pyrimidin-2-one 7, is reported. Addition of substituted 2-aminopyridines 5 to activated alkynoates leads to the facile formation of a series of metabolically stable trifluoromethyl substituted pyrido1,2-a]pyrimidines under mild conditions. |
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