Chin. J. Org. Chem. ›› 2013, Vol. 33 ›› Issue (10): 2237-2243.DOI: 10.6023/cjoc201305039 Previous Articles     Next Articles

Notes

4-甲基-2-杂环-2,3-二氢苯并[f]-1,5-硫氮杂(艹卓)-3-羧酸乙酯及其还原产物的合成、晶体结构及抑菌活性的研究

田克情a, 刘晓欣b, 薛子桥b, 杨田b, 杜星琼c, 张萍b   

  1. a 河北化工医药职业技术学院化学与环境工程系 石家庄 050026;
    b 河北师范大学化学与材料科学学院 石家庄 050024;
    c 河北师范大学生命科学学院 石家庄 050024
  • 收稿日期:2013-05-24 修回日期:2013-06-10 出版日期:2013-10-25 发布日期:2013-06-21
  • 通讯作者: 张萍 E-mail:zhangpingp@sina.com
  • 基金资助:

    国家自然科学基金(No. 20972040)资助项目

Studies on the Synthesis, Crystal Structure and Antimicrobial Activities of 4-Methyl-2-heterocylic-2,3-dihydro-benzo[f]-1,5-thiazepine-3-carboxylic Acid Ethyl Ester and Its Reduction Products

Tian Keqinga, Liu Xiaoxinb, Xue Ziqiaob, Yang Tianb, Du Xingqiongc, Zhang Pingb   

  1. a Environment and Chemical Engineering, Hebei Chemical and Pharmaceutical College, Shijiazhuang 050026;
    b College of Chemistry, Hebei Normal University, Shijiazhuang 050024;
    c College of Life Science, Hebei Normal University, Shijiazhuang 050024
  • Received:2013-05-24 Revised:2013-06-10 Online:2013-10-25 Published:2013-06-21
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 20972040).

Starting from ethyl acetoacetate and substituted heterocyclic aldehyde, a series of new 4-methyl-2-heterocyclic-2,3-dihydro-benzo[f]-1,5-thiazepine-3-carboxylic acid ethyl esters (2a2l) were synthesized through 2-step reactions, and of which five compounds were reduced. The structures of the compounds were characterized by 1H NMR, IR, MS, elemental analysis and X-ray diffraction study. The crystal of compound 2a belongs to triclinic system, space group P-1. The antibacterical activities of the new compounds against B. subtilis, C. albicans and C. neoformans were evaluated by filter paper approach, and the results indicated that most of them showed antibacterical activities, especially the compound 2a prominent.

Key words: 1,5-benzothiazepine, heterocyclic, reduction, crystal structure, antibacterical activity