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À propos de : Solid-Phase Synthesis of 4(1H)-Quinolone and PyrimidineDerivatives Based on a New ScaffoldPolymer-Bound CyclicMalonic Acid Ester        

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  • Solid-Phase Synthesis of 4(1H)-Quinolone and PyrimidineDerivatives Based on a New ScaffoldPolymer-Bound CyclicMalonic Acid Ester
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  • An efficient method for the preparation of polymer-bound cyclic malonic acid ester starting fromMerrifield resin has been developed. Reaction of the resin-bound cyclic malonic acid ester withtriethyl orthoformate and subsequent double substitution with nucleophilic reagents, such asarylamine, urea, thiourea, 2-aminobenzothiazoles, or isothiosemicarbazones, afforded the corresponding polymer-bound substituted aminomethylene cyclic malonic acid esters, which upon thermaltreament led to 4(1H)-quinolones, 3-substituted uracils and thiouracils, 4H-pyrimido[2,1-b]benzothiazol-4-ones, and 1-(N-alkylidene or benzylideneamino)-1,6-dihydro-2-methylthio-6-oxo-pyrimidines, depending on the structures of the nucleophilic reagents.
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