Synthesis of ss-Arylacyl/ss-Heteroarylacyl-ss-alkylidene Malonates and Their Application in Substituted Pyridone Synthesis

[摘要]：A novel approach has been developed for the synthesis of beta-arylacyl/beta-heteroarylacyl-beta-alkylidine malonates in moderate to good yields by the reaction of Stork aryl and heteroaryl enamine with beta-chloroalkylidene malonates. The reaction involves conjugate (Michael) addition of Stork enamine on beta-chloroalkylidene malonates and elimination of chloride ion. These Michael adducts were utilized as intermediates for the synthesis of highly substituted 1,4-dialkyl-2-oxo-6-aryl/hetreoaryl-1,2-dihydro-pyridine-3-carboxylic acid ethyl esters via 5 + 1 ring annulation protocol.

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