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[123I]iodomethane, a main product in the synthesis of 5-[123I]iodo-6-nitroquipazine by iododestannylation

✍ Scribed by Yolanda Zea-Ponce; Ronald M. Baldwin; Richard A. Miliust; Venkatesalu Bakthavachalam; Robert B. Innis

Publisher
John Wiley and Sons
Year
1995
Tongue
French
Weight
404 KB
Volume
36
Category
Article
ISSN
0022-2135

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✦ Synopsis

Radioiodinated 5-iodo-6-nitroquipaz.ine (2-piperazinyl-5-icd~6-nitiuquinoline), a selective serotonin transporter radiotracer, can be prepared by the reaction of its N-t-BOC-5trimethylstannyl precursor with ['ZrJ or [lWJNaI in the presence of chloramine-T, followed by amine deprotection by heating under acidic conditions. However, the labeling reaction is associated with a large and consistent formation of a volatile radioactive reaction product [37 f 4% (n = 11) for 1231 and 40 f 4% (n = 3) for lug.

The purpose of these experiments was to characterize the volatile radioactive product and to examine the effect of reaction temperature on its foxmation. The volatile radioactive product was identified as [1"rJ or [lPaiodomethane by its trapping characteristics and by its retention time in two different HPLC systems. Changing the reaction temperam (22-124OC) did not have a significant effect in the amount of labeled iodomethane prcduced (n = 13).

The conditions chosen for the radioicdination and deprotection were: 50 pg precursor in MeOH, dry NaW, 50 pl0.02 M chloramine-T in glacial HOAcMeOH, heating at 90°C for 15 min, followed by deprotection with CF3CaH for 5-10 min at the same temperature.

Purificarion was achieved by solvent extraction and HPLC.

Radiochemical yiew for preparations Carred out at temperatures between 86OC and 124OC were 24 f 5% (n = 11) for [1W+ and 45 f 13% (n = 3) for 5-[1~rJiodo-fj-nimquipazine; radiochemical purity averaged 95 f 4% and 99 f 0% respectively.

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