已报道了一系列2,6-取代的8-乙基-5,8-二氢-5-氧攒吡啶[2,3-d]嘧啶类化合物的合成与抗菌活性。最近Hiroshi Koga等通过构效关系的研究,指出6-位氟取代的吡酮酸类化合物不仅扩大了抗菌谱,而且增强了抗菌作用。为了进一步了解其构效关系并筛选更有效的抗菌药物,我们从4-氟-3-硝基苯胺(Ⅳ)出发,合成了7-氨基-1-乙基-6-氟-1,4-二氢-4-氧掛喹啉-3-羧酸乙酯(Ⅸ)。 为了用最简便的方法得到(Ⅳ),我们企图用工业原料(Ⅰ)进行部分还原而获得。关 A series of 2,6-substituted 8-ethyl-5,8-dihydro-5-oxazino [2,3-d] pyrimidines have been reported for their synthesis and antibacterial activity. Recently, Hiroshi Koga et al., Through the study of the structure-activity relationship, pointed out that the 6-position fluorine-substituted pyruvic acid compounds not only broadened the antibacterial spectrum but also enhanced the antibacterial activity. In order to further understand the structure-activity relationship and screen more effective antimicrobial agents, we synthesized 7-amino-1-ethyl-6-fluoro-1,4- Dihydro-4-oxoquinoline-3-carboxylate (IX). In order to obtain (IV) in the simplest way, we attempted to obtain it by partial reduction of industrial raw materials (I). turn off