1,4-二氧喹醛酸酯合成及抑菌活性研究

Study on the Synthesis and Bacteriostasis of 1,4-dioxide Quinoline Aldehydes Esters

为了合成两种具有抑菌活性的1,4-二氧喹醛酸酯,即1,4-二氧喹喔啉-3-甲基-2-甲酸苯酯和1,4-二氧喹喔啉-3-甲基-2-甲酸肉桂酯,以苯并呋咱为原料,经Beirut反应、酯交换反应,合成了两种喹醛酸酯;1,4-二氧喹喔啉-3-甲基-2-甲酸苯酯合成产率为29.3%,1,4-二氧喹喔啉-3-甲基-2-甲酸肉桂酯合成产率为18.3%。两种1,4-二氧喹醛酸酯对大肠杆菌、金葡萄球菌、青霉菌和枯草杆菌均有明显的抑菌活性。通过测定产物的熔点和光谱分析证明系为所合成的目标产物。

Using benzofuroxan as raw material,two kinds of 1,4- dioxide quinoline aldehydes esters,1,4-dioxide quinoline- 3- methyl- 2- phenyl formate and 1,4- dioxide quinoline- 3- methyl- 2-cinnamylformate,were synthesized by Beirut reaction and ester exchange reaction. The yield of 1,4- dioxide quinoline- 3- methyl- 2- phenyl formate was 29. 3% and the yield of 1,4- dioxide quinoline- 3- methyl- 2- cinnamylformate was 18. 3%. Two kinds of 1,4- dioxide quinoline aldehyde ester have obvious antibacterial activity to Escherichia coli,Staphylococcus aureus,Penicillium sp. and Bacillus subtilis. It was proved that new compounds synthesized in experiment were target compounds by measuring the melting point and spectral analysis.