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Synthesis of 123I-and labelled 5-iodo-6-nitroquipazine

✍ Scribed by Chester A. Mathis; Joel D. Enas; Stephen M. Hanrahan; Eyup Akgün

Publisher
John Wiley and Sons
Year
1994
Tongue
French
Weight
455 KB
Volume
34
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

The syntheses of the potent and selective serotonin reuptake complex radioligands [^123^I]‐ and [^125^I]5‐iodo‐6‐nitroquipazine (5‐iodo‐6‐nitro‐2‐piperazinylquinoline) are reported. A seven step synthetic sequence provided the BOC‐protected 5‐tributyltin‐6‐nitroquipazine precursor for radioiodination. End of synthesis radioiodination yields of ∼40% for ^123^I and ∼60% for ^125^I were achieved resulting in labelled products with high specific activities (>4000 and >2000 Ci/mmol, respectively) and radiochemical purities (>98%).

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