AN EXPEDIENT DOMINO CLICK APPROACH TO THE SYNTHESIS OF FACE ‘A’ 1,2,3-TRIAZOLO ANNULATED ANALOGUES OF 1,4-BENZODIAZEPINES OF MEDICINAL INTEREST
Journal Title: International Journal of Engineering and Science Invention - Year 2018, Vol 7, Issue 2
Abstract
The present work describes a concomitant formation of the 1,2,3 –triazole and 1,4- benzodiazepine rings in one step through a domino process by bringing an alkyne appended fragment in close proximity to the azide function to allow it to undergo a 1,3 dipolar cycloaddition reaction , to produce face „a‟ 1,2,3-triazolo annulated 1,4-diazepines . This concept of synthesis has been applied to 2-[2‟-imino methylene ethyne]-3-azido substituted derivative of 1,4-benzodiazepines and indole, to deliver the face „a‟ 1,2,3- triazolo annulated analogues of 1,4-diazepino condensed benzodiazepines3 and indoles. The 3-azide derivatives was in turn prepared by the diazotization of corresponding amine with [bmim]NO2 ionic liquid, in presence of HCl, followed by its treatment with [bmim]N3 ionic liquid, [bmim] = 1-benzyl-3-methyl imidazolium chloride. The noteworthy feature of this reaction was that it facilitated the formation of products in environmentally benign solvent free aqueous medium. The compounds were evaluated the anti-oxidant and anti-microbial activities.
Authors and Affiliations
Venkata Naga Baji Tokala
Keywords
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