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Journal of the Korean Chemical Society (JKCS)

ISSN 1017-2548(Print)
ISSN 2234-8530(Online)
Volume 55, Number 4
JKCSEZ 55(4)
August 20, 2011 

 
Title
Silica Sulfuric Acid as a Mild and Efficient Reagent for the Synthesis of 1,4-Diazepine and 1,5-Benzodiazepine Derivatives

Silica Sulfuric Acid를 이용한 효율적인 1,4-diazepine and 1,5-benzodiazepine 유도체의 합성
Author
Y C Joshi*, Shalini Saingar, Kavita, P Joshi, Rajesh Kumar

Y C Joshi*, Shalini Saingar, Kavita, P Joshi, Rajesh Kumar
Keywords
3H-1,5-Benzodiazepines, 1H-1,4-Diazepines, Ethylenediamine, o-Phenylenediamine, Silica sulfuric acid , 3H-1,5-Benzodiazepines, 1H-1,4-Diazepines, Ethylenediamine, o-Phenylenediamine, Silica sulfuric acid
Abstract
Silica sulfuric acid (SSA)를 이용하여 ethylenediamine (EDA)과 o-phenylenediamine (o-PDA)을 2-(4-methylthio benzenesulfonyl)- 1,3-dimethyl/1-methyl-3-phenyl/1,3-diphenyl/1-methyl-3-ethoxypropane-1,3-dione 3a-d과의 헤테로고리화 반응을 통하 여 좋은 생리활성을 나타내는1H-1,4-diazepines 4a-d과 3H-1,5-benzodiazepines 5a-d을 좋은 수율로 합성하였다. 이 반응에 서 β-diketones/β-ketoesters 3a-d는 4-methylthiobenzenesulfonyl chloride 1과 다양한 β-diketones/β-ketoesters 2a-d과의 축합반 응으로 합성하였으며, 합성한4a-d와 5a-d 화합물들에 대해서 fantimicrobial, antifungal 및anthelmintic 활성을 측정하였다.

The synthesis of biologically active 1H-1,4-diazepines 4a-d and 3H-1,5-benzodiazepines 5a-d in good yields, from the heterocyclization reaction of 2-(4-methylthio benzenesulfonyl)-1,3-dimethyl/1-methyl-3-phenyl/1,3-diphenyl/1-methyl-3- ethoxy propane-1,3-dione 3a-d with ethylenediamine (EDA) and o-phenylenediamine (o-PDA), respectively, in the presence of silica sulfuric acid (SSA) is described. The novel β-diketones/β-ketoesters 3a-d were synthesized by the condensation reaction of 4-methylthiobenzenesulfonyl chloride 1 with various β-diketones/β-ketoesters 2a-d. All structures of the newly synthesized compounds were elucidated by elemental analysis and spectral studies. The compounds 4a-d and 5a-d have been screened for antimicrobial, antifungal and anthelmintic activity.

Page
638 - 643
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