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

Document Type

Article

Publication Date

10-1-2006

Abstract

This paper describes the preparation of N,N'- diethyl - 6 - chloro - (4'- iodophenyl) - imidazo-[l,2 - a] pyridine - 3 -acetamide (CLINDE) and [131I] - labelled ([131I]- CLINDE). Non - radioactive imidazo[l,2-a]pyridine was synthesized by condensation of 5-chloro-2-aminopyridines with the bromo keto amides. Radiolabelling [131I]-imidazo [l,2 - a]pyridines was prepared by iododestannylation with Na[131I] in the presence of peroxide of hydrogen and purified by Ci18reverse phase HPLC. Non-radioactive imidazo-[l,2-a] pyridine was synthesized at a total yield of 30.8%. Radiolabelling [131I]-imidazo [l,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-[l,2-a]pyridine-3-acetamide and its radiosynthesis.

Publication Source (Journal or Book title)

He Jishu/Nuclear Techniques

First Page

777

Last Page

781

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