2,2二噻吩乙酸新席夫碱、1,3-恶氮平和四唑的合成、表征及生物活性研究

E. M. Hussain, Hussam Z. Naji
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引用次数: 1

摘要

本研究以1摩尔二氯乙酸和2摩尔噻吩为原料,合成了希夫碱5-8、1,3-恶氮平9-16和四唑17-19的新衍生物。以H2SO4为催化剂,分别以化合物1与甲醇或乙醇反应合成酯2-3,然后以2或3与水合肼80%反应合成2,2-二噻吩乙酰肼4。在干苯中,席夫碱与马来酸酐和邻苯二甲酸酐反应得到1,3-恶氮杂氮衍生物9-16,与叠氮化钠在四氢呋喃中反应得到四唑衍生物17-19。所有化合物都通过熔点、FTIR、1HNMR和化合物1、5和18的质谱进行了表征。对衍生物6、7、11、16、17和18进行抑菌试验。金黄色葡萄球菌等均被基金活跃。方案(1)。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis , Characterization and Study of Biological Activity of Some New Schiff Bases ,1,3-Oxazepine and Tetrazole Derived from 2,2 di thiophenyl Acetic Acid
In this study  new  derivatives  of  Schiff bases 5-8 , 1,3- oxazepine  9-16 and tetrazoles 17-19 have  been synthesized from the new starting  material 1 which has  synthesized  the reaction of  one mole of dichloro acetic acid and two moles of  thiophenol , the esters  2-3 were synthesized from the reaction of  compound 1 with methanol or ethanol respectively  in the presence of  H2SO4  as  catalyst  then 2,2-dithiophenylaceto Hydrazide  4 were synthesized from the reaction of  2 or 3 with hydrazine hydrate  80 % , Schiff bases 5-8 were  synthesized from the reaction of  4 with appropriate aldehyde or ketone .Treatment  of  Schiff bases with maleic and phathalic  anhydride in dry benzene to give 1,3-oxazepen derivatives  9-16 and with sodium azide in tetrahydrofuran (THF) afforded  tetrazole derivatives 17-19. All these compounds have been characterized from their melting pointes, FTIR , 1HNMR and compounds 1,5 and 18 by mass spectrometry . Derivatives 6,7,11,16,17 and 18 were tested against inhibition of E.coli and. Staphylococcus- aureus and were all funds to be active. Scheme (1).
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