A Novel Process for Synthesis of Imidazo-[ 1, 2-a ] Pyridine Ligand as the Peripheral Benzodiazepine Receptors

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 科研与新药推进处

	A Novel Process for Synthesis of Imidazo-[ 1, 2-a ] Pyridine Ligand as the Peripheral Benzodiazepine Receptors
	Li Jianfeng2 ; Huang Gang 3
刊名	Acta Universitatis Medicinalis Secondae Shanghai
	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
内容类型	期刊论文
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.