Journal
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
Volume 66, Issue 1, Pages 22-30Publisher
WILEY
DOI: 10.1002/jlcr.4009
Keywords
bioorthogonal; click chemistry; idodine-125; pretargeting; tetrazine
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Pretargeting imaging has gained attention for its excellent bioorthogonality and improved imaging contrast compared to conventional imaging. A new iodo tetrazine derivative has been synthesized and developed into an iodine-125 analog. Radiolabeling with N-chlorosuccinimide or chloramine-T in MeCN or MeOH resulted in a radiochemical conversion of >80%. Deprotection was successful when the radiolabeled tetrazine was stirred in 6-M HCl(aq.) at 60 degrees C for 2.5 h. This is the first iodine-labeled H-tetrazine. In vivo investigations on its pretargeting ability are currently underway.
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 (I-125) 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 degrees 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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