Synthesis of a DOTA--biotin conjugate for radionuclide chelation via Cu-free click chemistry

Org Lett. 2010 May 21;12(10):2398-401. doi: 10.1021/ol100774p.

Abstract

A strain-induced copper-free click reaction mediated by a new and easily prepared cyclooctyne derivative was used to efficiently assemble a DOTA-biotin adduct capable of radionuclide ((68)Ga) uptake. This synthetic strategy offers a potentially general and convenient means of preparing targeted radiolabeling and radiotherapeutic agents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biotin / chemistry*
  • Chelating Agents / chemical synthesis*
  • Chelating Agents / chemistry
  • Cyclooctanes / chemical synthesis*
  • Cyclooctanes / chemistry
  • Heterocyclic Compounds, 1-Ring / chemistry*
  • Molecular Structure
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / chemistry

Substances

  • Chelating Agents
  • Cyclooctanes
  • Heterocyclic Compounds, 1-Ring
  • Radiopharmaceuticals
  • 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
  • Biotin