摘要
以 2 ,4-二氯 -5 -氟苯乙酮为原料 ,通过β -酮酸酯化 ,与原甲酸三乙酯缩合 ,同 2 -氨基嘧啶发生取代反应 ,再经环合、硼络合和哌嗪化反应合成得到了N -嘧啶取代喹诺酮抗菌化合物 ,总收率为 2 2 .4% ,并研究了其抗菌活性。
N-pyrimidine quinolone derivative was synthesized from 2,4-dichloro-5-fluoroaceto phenone through β-keto-ester formation, condensation with triethyl orthoformate, substitution with 2-aminopyrimidine, cyclization, chelation with boric acid in acetic anhydride and followed by nucleophilic substitution reaction with piperazine. The total yield was 22.4%. Then the in vitro antibacterial activity against S.aureus and E.coli was tested.
出处
《湖北师范学院学报（自然科学版）》
2004年第3期22-24,共3页
Journal of Hubei Normal University(Natural Science)
关键词
喹诺酮化合物
合成
抗菌活性
quinolone derivative
synthesis
antibacterial activity
