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11C labelling of AG957—a potential tyrphostin radiotracer for PET

✍ Scribed by Uwe Ackermann; Henri J. Tochon-Danguy; Kenneth Young; John I. Sachinidis; J. Gordon Chan; Andrew M. Scott

Publisher
John Wiley and Sons
Year
2002
Tongue
French
Weight
140 KB
Volume
45
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Carbon‐11 labelled 4‐(N‐2,5‐dihydroxybenzyl)amino methyl benzoate (AG957), a potential radiotracer for imaging bcr–abl receptors was synthesized. [^11^C]AG957 was prepared by labelling 4‐aminobenzoic acid using [^11^C]CH~3~I, which affords the corresponding [^11^C] methyl ester in excellent yields. Subsequent condensation of the amino group with 2,5‐dihydroxy‐benzaldehyde formed the respective Schiff base. Reduction of this compound with NaBH~3~CN gave [^11^C]AG957 in overall decay corrected radiochemical yield of 65–75% (based on ^11^CH~3~I) with an average specific radioactivity of 40 GBq/μmol (1.1 Ci/μmol). The total synthesis time from EOB including formulation was 45 min. At physiological pH, the compound was found to be sufficiently stable for in vitro and in vivo investigations. Copyright © 2002 John Wiley & Sons, Ltd.

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