Synthesis and antimicrobial activity of 2-(3', 5'-disubstituted-indoly-2'-yl)-4H-3, 1-benzoxazin-4-ones and their derivatives

As benzoxazin-4-ones and quinazolines linked to indole nucleus acting as a good pharmacophore, the synthesis of these compounds has significant meaning. The key intermediates 2-(2', 5'-disubstituted-indol-2'-yl)-4H-3, 1-benzoxazin-4-ones (3) were synthesized from cyclocondensation of indole-2-carbon...

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Veröffentlicht in:化学与化工 2009 (12), p.54-59
1. Verfasser: Saundane A. R. Yarlakatti Manjunatha
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description As benzoxazin-4-ones and quinazolines linked to indole nucleus acting as a good pharmacophore, the synthesis of these compounds has significant meaning. The key intermediates 2-(2', 5'-disubstituted-indol-2'-yl)-4H-3, 1-benzoxazin-4-ones (3) were synthesized from cyclocondensation of indole-2-carbonyl chlorides (2) and anthranilic acid. Compound (3) on reaction with thiosemicarbazide and o-phenylene diamine afforded the compound (4) and (6) respectively. Compound (4) subjected to intramolecular cyclization under thermal conditions above its melting point afforded the compound (5). Similarly compound (3) on fusion with o- phenylene diamine gave compound (7). Structures of these compounds were confirmed by their spectral studies. The compounds were screened for their antimicrobial activity and the results were reported.
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subjects 二取代
化合物
合成
抗菌活性
苯并恶嗪
衍生物
邻氨基苯甲酸
邻苯二胺
title Synthesis and antimicrobial activity of 2-(3', 5'-disubstituted-indoly-2'-yl)-4H-3, 1-benzoxazin-4-ones and their derivatives
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