3-CH_2CH_2COOCH_3取代的1,5-苯并硫氮杂衍生物的合成、晶体结构及抑菌活性研究

Synthesis,Crystal Structure and Antibacterical Properties of 3-CH_2CH_2COOCH_3 Substituted 1,5-Benzothiazepines

从不同取代的苯出发,经5步反应合成了一系列3-CH2CH2COOCH3取代的1,5-苯并硫氮杂衍生物.化合物的结构经IR,1H NMR,13C NMR,MS和元素分析确证,并用X射线单晶衍射测定了化合物5f的晶体结构,证实了分子中的七元杂环是类船式构象.初步的抑菌活性测试结果表明,化合物5f和5h对枯草芽孢杆菌和临床新生隐球菌有微弱的抑制作用.

Starting from substituted benzenes, a series of 3-CH2CH2COOCH3 substituted 1,5-benzothi- azepines were synthesized through 5-step reactions. The structures of the new products were confirmed by IR, 1H NMR, 13C NMR, MS techniques and elemental analysis. The crystal structure of the compound 5f has been deterimined by X-ray diffraction analysis and the conformation of the seven-membered heterocycle is boat-like. The preliminary antibacterical experimental results showed that 5f and 5h have weak activities to Bacillus subtilis and Cryptococcus neoformansis.