BEHAVIOUR OF beta-KETO-delta-CARBETHOXYPHOSPHONATES AND PHOSPHINE OXIDES IN THE BIGINELLI MULTICOMPONENT REACTION: REGIOSELECTIVE SYNTHESIS OF 5-CARBETHOXY-6-PHOSPHONOMETHYL-3,4-DIHYDROPYRIMIDIN-2-ONES

[摘要]：An efficient one-pot synthesis of the novel 5-carbethoxy-6-phosphonomethyl-3,4-dihydropyrimidin-2-ones via a three-component Biginelli-type condensation of beta-keto-delta-carbethoxyphosphonates and phosphine oxides with aldehydes and urea in the presence of a catalytic amount of acetic acid, is described. The reaction proceeded efficiently at room temperature to afford regioselectively the title compounds in good to high yields. The factors governing the regioselectivity of the reaction are discussed.

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