外周苯二氮卓受体示踪剂^(131)I-CLINDE的合成和标记

Synthesis and iodine-radiolabelling of peripheral benzodiazepine receptor tracer ^(131)I-CLINDE

本文报道CLINDE改进的合成方法及其同位素131I-标记。标记前体由5-氯-2-氨基吡啶与溴代酮酰胺缩合制得。标记产物经三烷基锡化、过氧化氢-碘脱锡化而得。产物经反向HPLC分离纯化。结果显示,标记前体总收率30.8%,标记物放化得率80%,TLC和HPLC检测放化纯度大于98%。表明该法简便易行,放化得率好,产物纯度(包括放射化学纯度)高。

This paper describes the preparation of N,N＇-diethyl-6-chloro-（4＇-iodophenyl）-imidazo-[1,2-a] pyridine-3-acetamide （CLINDE） and [^131I]- labelled （^131I]- CLINDE）. Non-radioactive imidazo[1,2-a]pyridine was synthesized by condensation of 5-chloro-2-aminopyridines with the bromo keto amides. Radiolabelling [^131I]- imidazo [1,2-a]pyridines was prepared by iododestannylation with Na[talI] in the presence of peroxide of hydrogen and purified by C18 reverse phase HPLC. Non-radioactive imidazo-[1,2-a] pyridine was synthesized at a total yield of 30.8%. Radiolabelling [^131I]-imidazo [1,2-a]pyridines was prepared with a radiochemical yield of 80% and a radiochemical purity of greater than 98%. An improved, economical process is suited for preparing N, N＇-diethyl-6-chloro-（4＇-iodo-phenyl）-imidazo-[1,2-a]pyfidine-3 -acetamide and its radiosynthesis.