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Synthesis,Bioactivity and Crystal Structure Analysis of 2-(Benzo [d]isothiazol-3-yloxy)-N-(3-cyano-l-(4- fluorophenyl)-lH-pyrazol-5-yl) Acetamide
作者姓名:YU Peng,  LI Xi,  HU Jun,  XU Yan-Hua
作者单位:[1]College of Biotechnology and Pharmaceutical Engineering, Nanjing University of Technology, Nanjing 210009, China; [2]College of Environment, Nanjing University of Technology, Nanjing 210009, China; [3]Jiangsu Key Laboratory of Industrial Water-conservation & Emission Reduction, Nanjing 210009, China; [4]Post-doctoral Research Station of Chemical Engineering and Technology, Nanjing University of Technology, Nanjing 210009, China
基金项目:The generous financial support of this work from 2011 Key projects of Natural Science of Jiangsu province-owned colleges (No. 11YdA610001), Innovation project designated for graduate students of Jiangsu province (No. CXZZ13_0452), and the Postdoctoral research funding plan of Jiangsu province (No. 1202106C)
摘    要:A novel benzisothiazolin-3-one derivative, 2-(benzo[d]isothiazol-3-yloxy)-N-(3- cyano-l-(4-fluorophenyl)-lH-pyrazol-5-yl) acetamide (8), was synthesized from the initial compound benzo[d]isothiazol-3(2H)-one (BIT) 1 and 4-fluoroaniline 3. The structure of the target compound 8 was determined by elemental analyses, IR and 1H NMR. The single crystals of intermediate compound 6 and the target compound 8 were obtained and determined by X-ray diffraction analysis. The preliminary biological activity was also evaluated and the results showed tile target compound exhibited a good anti-microbial activity.

关 键 词:抗微生物活性  晶体结构  氟苯胺  乙酰胺  苯基  噻唑  合成  吡唑
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