A Novel Process for Synthesis of Imidazo-[ 1, 2-a ] Pyridine Ligand as the Peripheral Benzodiazepine Receptors
文献类型：期刊论文
| 作者 | Li Jianfeng2 ; Huang Gang3
|
| 刊名 | Acta Universitatis Medicinalis Secondae Shanghai
 |
| 出版日期 | 2005 |
| 卷号 | 25期号:12页码:1242-1245 |
| 关键词 | 125Ⅰ ^125I imidazo-[ 1,2-a] pyridines synthesis peripheral benzodiazepine receptors iododestannylation |
| ISSN号 | 0258-5898 |
| 其他题名 | 咪唑并吡啶类外周苯二氮卓受体配体的合成新方法 |
| 文献子类 | Article |
| 英文摘要 | Objective A novel process for synthesis of substituted imidazo-[ 1,2-a] pyridine and iodine-125 labelling as potential probes for the study of the peripheral benzodiazepine receptors was illustrated. Methods Non-radioactive imidazo-[ 1,2-a] pyridine was synthesized by condensation of 5-chloro-2-aminopyridines with the bromo keto esters and dialkylamines. The starting bromo keto esters were prepared by Friedel-Crafts acylation, esters and bromination. Radiolabelling ^125I-imidazo-[ 1, 2-a] pyridines was prepared by iododestannylation with Na ^125I in the presence of chloramine-T and purified by C18 reverse phase HPLC. Results Non-radioactlve imidazo-[ 1, 2-a] pyridine was synthesized in a total yield of 25.2%. Radiolabelling ^125I-imidazo-[ 1,2-a] pyridines was prepared in 68% radiochemical yield and over 98% radiochemical purity. Conclusion This novel process for preparation and radiosynthesis of imidazo-[ 1,2-a]-pyridine-3-acetamides are simple and with high recovery rate. |
| 资助项目 | 上海市教委重点发展基金[00000000] ; 上海市卫生局百人计划资助项目[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy ; General & Internal Medicine (provided by Clarivate Analytics) |
| 语种 | 中文 |
| CSCD记录号 | CSCD:2204298 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/268282]  |
| 专题 | 科研与新药推进处 |
| 作者单位 | 1.Reiji Hospital, Shanghai Second Medical University, Shanghai 200127, China.; 2.Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences. 3.Department of Nuclear Medicine, Reiji Hospital, Shanghai Second Medical University, Shanghai 200127, China.; |
| 推荐引用方式 GB/T 7714 | Li Jianfeng,Huang Gang. A Novel Process for Synthesis of Imidazo-[ 1, 2-a ] Pyridine Ligand as the Peripheral Benzodiazepine Receptors[J]. Acta Universitatis Medicinalis Secondae Shanghai,2005,25(12):1242-1245. |
| APA | Li Jianfeng,&Huang Gang.(2005).A Novel Process for Synthesis of Imidazo-[ 1, 2-a ] Pyridine Ligand as the Peripheral Benzodiazepine Receptors.Acta Universitatis Medicinalis Secondae Shanghai,25(12),1242-1245. |
| MLA | Li Jianfeng,et al."A Novel Process for Synthesis of Imidazo-[ 1, 2-a ] Pyridine Ligand as the Peripheral Benzodiazepine Receptors".Acta Universitatis Medicinalis Secondae Shanghai 25.12(2005):1242-1245. |
入库方式： OAI收割
来源：上海药物研究所
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