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Synthesis of a DOTA--biotin conjugate for radionuclide chelation via Cu-free click chemistry
Journal article   Peer reviewed

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

Michael K Schultz, Sharavathi G Parameswarappa and F Christopher Pigge
Organic letters, Vol.12(10), pp.2398-2401
05/21/2010
DOI: 10.1021/ol100774p
PMCID: PMC5506828
PMID: 20423109
url
http://doi.org/10.1021/ol100774pView
Open Access

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

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