4.7 Article

Green route for the heterocyclization of 2-mercaptobenzimidazole into β-lactum segment derivatives containing -CONH- bridge with benzimidazole:: Screening in vitro antimicrobial activity with various microorganisms

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 14, Issue 24, Pages 8271-8279

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2006.09.017

Keywords

2-azetidinones; heterocyclization; microwave effect; antimicrobial interest

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The efficient and rapid synthesis of novel azetidin-2-ones 4a-j has been established. Thus, both microwave and conventional condensation 2-{(1H-benzimidazol)-ylthio}-N'-2-(substituted phenyl) hydrazide with chloroacetylchloride were carried out in DMF-benzene solvent in the presence of Et3N catalyst. The microwave synthesis route afforded better yield with short time. The novel heterocycles were characterized by elemental analysis and spectral features. Some of the produced compounds were screened for their antimicrobial activity. (c) 2006 Elsevier Ltd. All rights reserved.

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