4.7 Article

Alumina-supported synthesis of antibacterial quinolines using microwaves

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BIOORGANIC & MEDICINAL CHEMISTRY
卷 8, 期 1, 页码 69-72

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0968-0896(99)00256-4

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support; quinoline; drymedia; basic alumina; microwaves; solid support

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7-(5'-Alkyl-1',3',4'-thiadiazol/oxadiazol-2'-ylthio)-6-fluoro-2,4-dimethylquinolines and 3-formyl-2-(2'-hydroxy-1',4'-naphthoquinon-3'-yl)-4-melhyl/6-methyl/7 have been synthesised by the reaction of 5-alkyl-1,3,3-thiadiazol/oxadiazol-2-thiols with 7-chloro-6-fluoro-2,4-dimethylquinoline and by the reaction of 2-hydroxy-1,4-naphthoquinone with 2-chloro-3-formyl-4-methyl/6-methyl/7-methyl/8-methylquinoline respectively on basic alumina using microwaves, the reaction time has been brought down from hours to seconds with improved yield as compared to conventional heating. The compounds were tested for their in vitro antibacterial activity. All compounds showed promising antibacterial activity. The best activity was observed by compounds 3a and 3f. (C) 2000 Elsevier Science Ltd. All rights reserved.

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