含三唑啉硫酮槟榔碱衍生物的合成和生物活性 |
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引用本文: | 胡国强,黄文龙,张惠斌,汪海. 含三唑啉硫酮槟榔碱衍生物的合成和生物活性[J]. 有机化学, 2002, 22(9): 667-671 |
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作者姓名: | 胡国强 黄文龙 张惠斌 汪海 |
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作者单位: | 1. 中国药科大学新药研究中心,南京,210009 2. 军事医学科学院毒物药物研究所,北京,100850 |
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基金项目: | 国家重点基础研究发展 (No.G19980 5 1112 )规划项目 |
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摘 要: | 烟酸经酯化、肼解、与取代芳酸异硫氰酸酯缩合成 1 (3 吡啶甲酰基 ) 4 芳基氨基硫脲 (2 ) ,2经环合生成 2 (3 吡啶 ) 4 芳基 1,3,4 三唑啉 5 硫酮 (3) ,接着用碘甲烷对吡啶环季铵化得相应的季铵盐 4 ,4用硼氢化钠还原可得目标物 2 (1 甲基 1,2 ,5 ,6 四氢吡啶 3 基 ) 4 芳基 1,2 ,4 三唑啉 5 硫酮 (5 ) .对所合成的目标化合物进行了舒张血管活性实验
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关 键 词: | 1 2 4-三唑啉 槟榔碱衍生物 合成 血管舒张活性 |
修稿时间: | 2001-09-25 |
Synthesis and Bioactivity of Arecoline Derivatives Containing 1,2,4-Triazone |
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Abstract: | 1-Nicotinyl 4 arylthiosemicarbazides (2) were synthesized by condensation of substituted aryl isothiocynates with nicotinic acid hydrazide. Cyclization of 2 in the presence of sodium hydroxide (2 mol/L) resulted in 2 (3 pyridyl) 4 aryl 1,2,4 triazoline 5 thione (3). The resulting triazolothiones 3 were treated with methyl iodide to give corresponding methyl pyridinium salts 4 which was then reduced with sodium borohydride to afford the title compounds of 2 (1 methyl 1,2,5,6 tetrahydropyridin 3 yl) 4 aryl trazoline 5 thiones (5). This method has been utilized in the synthesis of muscarinic agonist candidates. |
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Keywords: | 1 2 4-triazoline arecoline derivatives synthesis bioactivity |
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