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

• 作者: Babasaheb V. Kendre Mahadev G. Landge Sudhakar R. Bhusare
• 来源期刊: 药物化学期刊(英文)
• 学科: 化学
• 关键词: ALDIMINE Azetidin-2-One ANTI-INFLAMMATORY p-Amino Benzoic Acid 2-Amino Pyridine p-Toluene Sulfonyl Chloride
• 年，卷（期）: 2012,（3）
• 页码范围: 98-104
• 页数: 7页
• 分类号: O6

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.