吡啶2,3-d)嘧啶类抗菌物质的研究
STUDIES ON PYRIDO (2,3-d) PYRIMIDINE ANTIBACTERIAL AGENTS
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摘要: 本文报道了一系列2,6-取代的5,8-二氢-8-乙基-5-氧吡啶2,3-d嘧啶类化合物的合成和抗菌活性,并确证2-氯-4-(2’-甲氧羰基二乙氨基)嘧啶-5-羧酸乙酯Ⅳ经过Dieckmann环化所得的产物为2-氯-7,8-二氢-8-乙基-5-羟基吡啶2,3-d嘧啶-6-羧酸甲酯Ⅴ,即以烯醇式存在,而不是以Pesson等氏报道的酮式结构Ⅵ存在。Abstract: The synthesis and antibacterial activity of a series of 2,6-substituted 5,8-dihydro-8-ethyl-5-oxopyrido (2,3-d)pyrimidine are reported. The product from ethyl 2-chloro-4-(2-methoxycarbonyldiethylamino) pyrimidine-5-carboxylate (Ⅳ) through Dieckmann cyclization is determined as methyl 2-chloro-7,8-dihydro-8-ethyl-5-hydroxypyrido (2,3-d) pyrimidine-6-carboxylate (Ⅴ). It exists in the enol form, not the keto form (Ⅵ) as reported by Pesson.
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