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以乙酰乙酸乙酯和含不同取代基的杂环醛为原料,经两步反应合成了一系列新颖的4-甲基-2-杂环-2,3-二氢苯并[f]-1,5-硫氮杂-3-羧酸乙酯(2a~2l),并对其中的5个化合物进行了还原,2a~2l及还原产物的结构经1H NMR IR,MS,元素分析确证.同时采用X射线衍射法测定了2a的晶体结构,2a属三斜晶系,P-1空间群.采用滤纸片法测试所合成目标化合物对枯草芽孢杆菌、白色念珠菌、标准新生隐球菌和临床新生隐球菌的抑菌活性,结果表明大部分化合物都有一定的抑菌效果,其中2a的抑菌效果尤其突出.
A series of novel 4-methyl-2-hepto-2,3-dihydrobenzo [f] -1-heptanone derivatives were synthesized via two steps using ethyl acetoacetate and heterocyclic aldehydes with different substituents as starting materials , 5-thiazepine-3-carboxylic acid ethyl ester (2a ~ 2l). Five of these compounds were reduced. The structures of 2a ~ 2l and the reduction products were confirmed by 1H NMR, MS and elemental analysis. The crystal structure of 2a, 2a triclinic system and P-1 space group were also determined by X-ray diffraction.The target compound was tested for its activity against Bacillus subtilis, Candida albicans, Cryptococcus neoformans and clinical The antibacterial activity of Cryptococcus neoformans, the results show that most of the compounds have a certain antibacterial effect, of which 2a antibacterial effect is particularly prominent.