The ^14^C labelling of three compounds : HI‐6, TMB‐4 and pyrimidoxime is described from ^14^C‐formic acid, sodium salt. The compounds were prepared by lithiation and formylation with N‐methyl (^14^C)‐formanilide followed by introduction of the hydroxylamine moieties and alkylation of the pyridine. R
Marquages par [14C] et [13C] de la N-(2-diéthylaminoéthyl)-4-iodobenzamide et de la N-(3-diméthylaminoprophyl)-4-iodobenzamide, traceurs du mélanome
✍ Scribed by M. F. Moreau; D. Parry; M. Bayle; J. Papon; P. Labarre; A. Veyre
- Publisher
- John Wiley and Sons
- Year
- 1995
- Tongue
- French
- Weight
- 468 KB
- Volume
- 36
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
N‐(2‐diethylaminoethyl)‐4‐iodobenzamide (I) and N‐(3‐dimethylaminopropyl)‐4‐iodobenzamide (II), recently developed in our laboratory, are promising agents for metastatic melanoma detection in nuclear medicine. In order to study their “in vivo” metabolism, we labelled them with carbon‐14 and carbon‐13 on two sites: on the carbonyl group (Ia, IIa), and on the dialkylaminoalkyl moiety (Ib, IIb). The overall yields calculated from sodium [^14^C] or [^13^C] cyanide used as precursor are in the range of 55% for Ia, IIa, IIb, and 21% for Ib.
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The two compounds were labelled by ^14^C on the hydroxyimino methyl group substituted on the 2 positions of the pyridinium ring. The convenient pyridinium lithiated intermediates were formylated with N‐methyl ^14^C‐formanilide. The hydroxyimino methyl groups were synthezised by reaction of the ^14^