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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 발행연도
- 2017.1
- 수록면
- 98 - 102 (5page)
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초록· 키워드
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We demonstrate a detail protocol for the radiosynthesis of a $^{125}I-labeled$ tetrazine prosthetic group and its application to the efficient radiolabeling of trans-cyclooctene-group conjugated human serum albumin (3) using inverse-electron-demand Diels-Alder reaction. Radioiodination of the stannylated precursor (2) was carried out by using [$^{125}I$]NaI and chloramine T as an oxidant at room temperature for 15 min. After HPLC purification of the crude product, the purified $^{125}I-labeled$ azide ([$^{125}I$]1) was obtained with high radiochemical yield ($65{\pm}8%$, n = 5) and excellent radiochemical purity (>99%). Inverse-electron-demand Diels-Alder reaction between ([$^{125}I$]1) and 3 gave the $^{125}I-labeled$ human serum albumin ([$^{125}I$]4) with more than 99% of radiochemical yield as determined by radio-thin-layer chromatography (radio-TLC). These results clearly indicate that the present radiolabeling method will be useful for the efficient and convenient radiolabeling of trans-cyclooctene-group containing biomolecules.
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