Solid-phase synthesis of pyrido[2,3-d]pyrimidin-7-ones |
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| Authors: | Mauro Angiolini Maria Menichincheri |
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| Institution: | Discovery Oncology, Nerviano Medical Sciences, viale Pasteur 10, 20014 Nerviano, Italy |
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| Abstract: | A novel solid-phase method for the synthesis of 4-methyl-pyrido2,3-d]pyrimidin-7-one compounds with two diversity points is described. The polymer supported methylsulfonyl derivatives A3, achieved by coupling compound G with different resin-bound amines A1 followed by oxidation with MCPBA, are substituted with several amines R1R2NH. Final cleavage affords 126 compounds having formula H in good yield and purity. |
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| Keywords: | Pyrido[2 3-d]pyrimidin-7-one Solid-phase Formyl resin Scaffold Library |
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