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Microwave Assisted and Al2O3/K2CO3 Catalyzed Synthesis of Azetidin-2-One Derivatives Containing Aryl Sulfonate Moiety with Anti-Inflammatory and Anti-Microbial Activity

Microwave Assisted and Al2O3/K2CO3 Catalyzed Synthesis of Azetidin-2-One Derivatives Containing Aryl Sulfonate Moiety with Anti-Inflammatory and Anti-Microbial Activity
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摘要 We report the novel synthesis of azetidin-2-one derivatives containing aryl sulfonate moiety from the reaction of 2-hydroxy benzaldehyde with p-toluene sulfonyl chloride afforded firstly 2-formylphenyl 4-methylbenzene sulfonate (2). The compound (2) on reaction with p-aminobenzoic acid or 2-aminopyridine gave the corresponding aldimines (3). Furthermore, the aldimines are on reaction with chloroacetyl chloride gives corresponding azetidin-2-ones in good to moderate yield. Among the eight synthesized azetidin-2-ones, five selected compounds have been screened for the an-ti-inflammatory activity, few of them showed good anti-inflammatory activity compared with standard drugs. Anti- microbial activity of all synthesized compounds has been tested and most of the compounds showed good anti-bacterial and anti-fungal activities. We report the novel synthesis of azetidin-2-one derivatives containing aryl sulfonate moiety from the reaction of 2-hydroxy benzaldehyde with p-toluene sulfonyl chloride afforded firstly 2-formylphenyl 4-methylbenzene sulfonate (2). The compound (2) on reaction with p-aminobenzoic acid or 2-aminopyridine gave the corresponding aldimines (3). Furthermore, the aldimines are on reaction with chloroacetyl chloride gives corresponding azetidin-2-ones in good to moderate yield. Among the eight synthesized azetidin-2-ones, five selected compounds have been screened for the an-ti-inflammatory activity, few of them showed good anti-inflammatory activity compared with standard drugs. Anti- microbial activity of all synthesized compounds has been tested and most of the compounds showed good anti-bacterial and anti-fungal activities.
出处 《Open Journal of Medicinal Chemistry》 2012年第3期98-104,共7页 药物化学期刊(英文)
关键词 ALDIMINE Azetidin-2-One ANTI-INFLAMMATORY p-Amino Benzoic Acid 2-Amino Pyridine p-Toluene Sulfonyl Chloride Aldimine Azetidin-2-One Anti-Inflammatory p-Amino Benzoic Acid 2-Amino Pyridine p-Toluene Sulfonyl Chloride
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