4-甲基-2-芳基(杂环基)-1,3-噻唑-5-甲酸乙酯的合成及抑菌活性研究

Synthesis and Antibacterial Activities of Ethyl-4-methyl-2-aryl-1,3-thiazole-5-carboxylate

以硫代芳基（杂环基）甲酰胺和2-氯乙酰乙酸乙酯为原料合成了4-甲基-2-芳基（杂环基）-1,3-噻唑-5-甲酸乙酯。于甲醇溶剂中,55℃至回流条件下,由腈与17%硫化铵溶液反应4~5 h制得硫代芳基（杂环基）甲酰胺中间产物。所合成的硫代酰胺及目标产物经IR、1HNMR、MS表征,其中4-甲基-2-（苯酞-5-基）-1,3-噻唑-5-甲酸乙酯尚未见报道,并分别测试了上述化合物对大肠杆菌（Escherichia coli）和枯草芽孢杆菌（Bacillus subtilis）的抑菌活性,结果表明部分化合物具有一定的抑菌活性。

2-Aryl（ heterocyclic group）-4-methyl-1,3-thiazole-5-carboxylate were synthesized viacyclization reaction of thioamide and 2-chloroacetoaceticacidethylester. Thioamide compounds were prepared from nitrile with ammonium sulfide in the presence of methanol as solvent at 55 ℃ for 4 ~ 5 h. The structures of target compounds were confirmed by IR,1HNMR and mass spectral studies,and the compound ethyl-2-（ benzenepeptide-5-yl）-4-rnethyl-1,3-thiazole-5-carboxylate are novel. Preliminary antibacterial experiments were tested,and the results indicated that some of the above compounds have good antibacterial activities.