A Three-Component Approach to 3,5-Diaryl-1,2,4-thiadiazoles under Transition-Metal-Free Conditions

作者：Xie, Hao; Cai, Jinhui; Wang, Zilong; Huang, Huawen^*; Deng, Guo-Jun^*

来源：Organic Letters, 2016, 18(9): 2196-2199.

DOI：10.1021/acs.orglett.6b00806

• VITRO ANTITUBERCULOSIS ACTIVITY
• OXIDATIVE DIMERIZATION
• 3,5-DISUBSTITUTED 1,2,4-THIADIAZOLES
• GASTRIC (H+/K+)-ATPASE
• REVERSIBLE INHIBITORS
• COUPLING REACTIONS
• ELEMENTAL SULFUR
• DERIVATIVES
• DESIGN
• AGENTS

A novel route is disclosed for the synthesis of 1,2,4-thiadiazoles starting from amidines, elemental sulfur, and 2-methylquinolines or aldehydes under transition-metal-free conditions. This three-component approach affords efficient and rapid access to 3,5-diaryl substituted 1,2,4-thiadiazoles with good tolerance of a broad range of funcitional groups. Mechanistic studies reveal a radical-involved pathway.

• 出版日期2016-5-6
• 单位湘潭大学