Synthesis and radiolabeling of a polar [125 I]I-1,2,4,5-tetrazine.
J Labelled Comp Radiopharm
; 66(1): 22-30, 2023 Jan.
Article
en En
| MEDLINE
| ID: mdl-36539610
ABSTRACT
Pretargeting imaging has gained a lot of prominence, due to its excellent bioorthogonality and improved imaging contrast compared to conventional imaging. A new iodo tetrazine (Tz) derivative has been synthesized and further developed into the corresponding iodine-125 (125 I) analog (12), via the trimethylstannane precursor. Radiolabeling with either N-chlorosuccinimide or chloramine-T, in either MeCN or MeOH proceeded with a radiochemical conversion (RCC) of >80%. Subsequent deprotection only proved successful, among the tested conditions, when the radiolabeled Tz was stirred in 6-M HCl(aq.) at 60°C for 2.5 h. To the best of our knowledge, this is the first H-tetrazine labeled with iodine. In vivo investigations on the pretargeting ability of 12 are currently under way.
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1
Colección:
01-internacional
Banco de datos:
MEDLINE
Asunto principal:
Radiofármacos
/
Compuestos Heterocíclicos
Idioma:
En
Revista:
J Labelled Comp Radiopharm
Año:
2023
Tipo del documento:
Article
País de afiliación:
Dinamarca