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Bioorg Med Chem. 2016 Apr 19; doi: 10.1016/j.bmc.2016.04.029. Epub 2016 Apr 19.

Highly efficient method for .

Bioorganic & medicinal chemistry

Mi Hee Choi, Ha Eun Shim, Seong-Jae Yun, Hye Rim Kim, Sajid Mushtaq, Chang Heon Lee, Sang Hyun Park, Dae Seong Choi, Dong-Eun Lee, Eui-Baek Byun, Beom-Su Jang, Jongho Jeon

Affiliations

  1. Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, Jeonbuk 56212, Republic of Korea.
  2. Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, Jeonbuk 56212, Republic of Korea; Department of Radiation Biotechnology and Applied Radioisotope Science, Korea University of Science and Technology, Deajeon 34113, Republic of Korea.
  3. Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, Jeonbuk 56212, Republic of Korea; Department of Radiation Biotechnology and Applied Radioisotope Science, Korea University of Science and Technology, Deajeon 34113, Republic of Korea. Electronic address: [email protected].
  4. Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongeup, Jeonbuk 56212, Republic of Korea; Department of Radiation Biotechnology and Applied Radioisotope Science, Korea University of Science and Technology, Deajeon 34113, Republic of Korea. Electronic address: [email protected].

PMID: 27134118 DOI: 10.1016/j.bmc.2016.04.029

Abstract

In this report, we present a rapid and highly efficient method for radioactive iodine labeling of trans-cyclooctene group conjugated biomolecules using inverse-electron-demand Diels-Alder reaction. Radioiodination reaction of the tetrazine structure was carried out using the stannylated precursor 2 to give

Copyright © 2016 Elsevier Ltd. All rights reserved.

Keywords: Bioorthogonal reaction; Inverse-electron-demand Diels–Alder reaction; Radioactive iodine; Radiolabeling; Radiotracer

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