摘要
An I-2-DMSO-mediated multicomponent [3+1+2]cascade annulationreaction using aryl methyl ketones, enaminones, and benzo[d]isoxazol-3-amine as substrates has been developed. Thismetal-free reaction involved the transannulation of benzo[d]isoxazol-3-amines with the formation of two C-Nbonds and a C-C bond in one pot. Notably, a pyrimidine ringwith a 1,4-dicarbonyl scaffold could efficiently transform into apyrimido[4,5-d]pyridazine skeleton. The phenolichydroxyl group of the target product could undergo further modificationwith pharmaceuticals, demonstrating the utility of this method.
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单位1; 广东医学院