Synthesis and radiolabeling of a polar [125 I]I-1,2,4,5-tetrazine
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Synthesis and radiolabeling of a polar [125 I]I-1,2,4,5-tetrazine. / Bidesi, Natasha; Shalgunov, Vladimir; Battisti, Umberto Maria; Hvass, Lars; Jørgensen, Jesper Tranekjaer; Poulie, Christian B M; Jensen, Andreas I; Kjaer, Andreas; Herth, Matthias M.
I: Journal of Labelled Compounds and Radiopharmaceuticals, Bind 66, Nr. 1, 2023, s. 22-30.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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TY - JOUR
T1 - Synthesis and radiolabeling of a polar [125 I]I-1,2,4,5-tetrazine
AU - Bidesi, Natasha
AU - Shalgunov, Vladimir
AU - Battisti, Umberto Maria
AU - Hvass, Lars
AU - Jørgensen, Jesper Tranekjaer
AU - Poulie, Christian B M
AU - Jensen, Andreas I
AU - Kjaer, Andreas
AU - Herth, Matthias M
N1 - © 2022 The Authors. Journal of Labelled Compounds and Radiopharmaceuticals published by John Wiley & Sons Ltd.
PY - 2023
Y1 - 2023
N2 - 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.
AB - 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.
U2 - 10.1002/jlcr.4009
DO - 10.1002/jlcr.4009
M3 - Journal article
C2 - 36539610
VL - 66
SP - 22
EP - 30
JO - Journal of Labelled Compounds and Radiopharmaceuticals
JF - Journal of Labelled Compounds and Radiopharmaceuticals
SN - 0362-4803
IS - 1
ER -
ID: 333698997