邻苯甲酰四氯苯甲酸及其三有机锡羧酸酯的合成表征和抑菌活性研究

目的合成邻苯甲酰四氯苯甲酸（C6H5COCl4C6H5CO2H1）及其三有机锡羧酸酯化合物C6H5COCl4C6H5CO2SnR（R=Ph,2a;R=Bz,2b;R=Cy,2c;R=C6H5C（CH3）2CH2,2d）,研究它们的抑菌活性。方法化合物1以四氯邻苯二甲酸酐经傅─克酰基化反应合成,化合物2a~2d由1与氢氧化锡在苯中加热回流制得。通过元素分析I、R和1HNMR表征了其结构,并利用微量量热法测试了它们对大肠杆菌的抑菌活性。结果与市售抗菌药比较,不论羧酸还是有机锡羧酸酯都有较强的杀菌活性,多数和青霉素相当。结论实验数据为探索高效、低毒的杀菌药物提供了具有参考价值的信息。

Synthesis,characterization and bacteriostatic power on escherichia coli of triorganotin 2-benzoyl-3,4,5,6-tetrachlorobenzoic carboxylates

Objective To synthesize 2-benzoyl-3,4,5,6-tetrachlorobenzoic acid（C6H5COCl4C6H5CO2H 1） and its triorganotin carboxylates C6H5COCl4C6H5CO2SnR（R=Ph 2a;R=Bz 2b;R=Cy 2c;R=C6H5C（CH3）2CH2 2d） and study their antibacterial activity.Methods Compound 1 was synthesized by Friedel-Crafts acylation from Tetrachlorophthalic anhydride and compound 2a~2d were synthesized using 1 and stannic hydroxide.Their structures were determined by elemental analysis,IR and ^1HNMR.Their bacteriostasic activity against Escherichia Coli was assayed by microcalorimetry.Results Bioassay results have revealed that the compounds possess good bacteriostasic activity against Escherichia Coli.Compared with Commercial antibacterial agents.Conclusion The experimental data provide good references for exploration of high efficient and low toxic antibiotics.