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A novel three-step entry toward phthalazine derivatives has been elaborated. A strategy based on a sequential acyl-alkylation/diazo transfer reaction/Diaza-Wittig reaction led to the desired analogues in moderate to good yields from an aryne precursor. Various aryl groups were introduced on the annulated pyridazine, moreover the presence of an ester group allows further modifications.
A convenient and selective synthesis of 6-substituted-4-hydroxy-3-methoxycarbonyl pyridazines has been developed via a diaza-Wittig reaction. The desired products substituted at the C6 position can be obtained from readily available starting materials under mild conditions. This represents an attractive new method for the synthesis of pyridazine derivatives.
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