TEBAB应用于诺氟沙星氯乙基化衍生物的合成研究

TEBAB applied to norfloxacin chlorine ethylation derivatives synthesis

以1,2-二氯乙烷和诺氟沙星为原料,TEBAB(三乙基丁基溴化铵)为相转移催化剂合成一种新型的、未见报道的诺氟沙星N-4′位氯乙基化衍生物,并测试了其抗菌活性。考察了反应温度、物料比和反应时间对该合成反应产率的影响。实验表明,当反应温度为70℃,n(诺氟沙星)∶n(二氯乙烷)=1.0∶1.4、反应时间为3h时,相转移催化剂TEBAB为0.2g,NaOH溶液质量分数5%,反应产率为72%左右。测试了新型的季铵盐类相转移催化剂TEBAB的活性。实验证明,新型季铵盐类相转移催化剂TEBAB的催化效果较好,活性较强。最后,经熔点测定和红外光谱表征确证合成产物为目的物,且产品抗菌活性较诺氟沙星有所提高。

This topic is studied with 1,2-dichloroethane and norfloxacin as raw material,TEBAB（triethyl ammonium butyl bromide）as phase transfer catalyst synthesis a new kind of,not seen reports of norfloxacin N-4 chlorination ethylation derivatives,and test its antibacterial activity.Testing the reaction temperature,material ratio and reaction time on the synthesis reaction yield,the influence of the experiments show that when the reaction temperature is 70 ℃,n（norfloxacin）/n（ethylene dichloride）of 1∶1.4,the reaction time is 3h,phase transfer catalyst TEBAB quantity 0.2g;5% NaOH solution concentration,the reaction yield about 72%.And test the new type of the activity of quaternary ammonium salt type of phase transfer catalyst TEBAB.Experiment proves that the new type quaternary ammonium salt phase transfer catalyst TEBAB catalytic effect is good,strong activity.Finally are confirmed by melting point measurement and ir characterization of synthetic products for the purpose.The norfloxacin improves product antibacterial activity.