引用本文:
Guo Qiang HU, Wen Long HUANG, Hai WANG. Synthesis of Tetrahydropyridinyltriazolothiadiazines as Possible Muscarinic Agonists[J]. Chinese Chemical Letters,
2005, 16(1): 1-3.
Citation: Guo Qiang HU, Wen Long HUANG, Hai WANG. Synthesis of Tetrahydropyridinyltriazolothiadiazines as Possible Muscarinic Agonists[J]. Chinese Chemical Letters, 2005, 16(1): 1-3.
Citation: Guo Qiang HU, Wen Long HUANG, Hai WANG. Synthesis of Tetrahydropyridinyltriazolothiadiazines as Possible Muscarinic Agonists[J]. Chinese Chemical Letters, 2005, 16(1): 1-3.
Synthesis of Tetrahydropyridinyltriazolothiadiazines as Possible Muscarinic Agonists
摘要:
4-Amino-5-(pyridin-3-yl)-4H-1,2,4-triazole-3-thiol 1 were condensed with 2-bromo-1-(substituted phenyl) ethanone to give pyridinyltriazolothiadiazines 2a~c, which were quaternarized with methyl iodide and oxidized with 30% hydrogen peroxide to afford the corresponding methyl pyridinium salts 3a~c and pyridine-l-oxides 4a~c, respectively. The reduction of compounds 3 and 4 with NaBH4 in methanol produced the target compounds 1-methyl-1, 2, 5, 6-tetrahydropyridin-3-yl)-6-aryl-s-triazolothiadiazines 5a~c and 3-(1-hydroxyl-1, 2, 5, 6-tetrahydropyridin-3-yl)-6-aryl-s-triazolothiadiazines 6a~c, respectively. The endothelium vascular relaxing activity of the target compounds was screened.
English
Synthesis of Tetrahydropyridinyltriazolothiadiazines as Possible Muscarinic Agonists
Abstract:
4-Amino-5-(pyridin-3-yl)-4H-1,2,4-triazole-3-thiol 1 were condensed with 2-bromo-1-(substituted phenyl) ethanone to give pyridinyltriazolothiadiazines 2a~c, which were quaternarized with methyl iodide and oxidized with 30% hydrogen peroxide to afford the corresponding methyl pyridinium salts 3a~c and pyridine-l-oxides 4a~c, respectively. The reduction of compounds 3 and 4 with NaBH4 in methanol produced the target compounds 1-methyl-1, 2, 5, 6-tetrahydropyridin-3-yl)-6-aryl-s-triazolothiadiazines 5a~c and 3-(1-hydroxyl-1, 2, 5, 6-tetrahydropyridin-3-yl)-6-aryl-s-triazolothiadiazines 6a~c, respectively. The endothelium vascular relaxing activity of the target compounds was screened.
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Key words:
- Tetrahydropyridine
- / triazolothiadiazine
- / muscarinic agonist
- / vascular activity.
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