Steroids labeled with 18F for imaging tumors by positron emission tomography

J. A. Katzenellenbogen

doi:10.1016/S0022-1139(01)00379-7

Steroids labeled with ¹⁸F for imaging tumors by positron emission tomography

J. A. Katzenellenbogen

Chemistry

Research output: Contribution to journal › Article › peer-review

Abstract

The chemistry to label radiopharmaceuticals for imaging with positron emission tomography (PET) with the 2 h half life positron-emitting radionuclide fluorine-18 (¹⁸F) requires ease, efficiency, and speed. Furthermore, when high specific activities are needed, as in imaging high affinity, low capacity receptors, reactions need to work well at the tracer level scale. This review covers ¹⁸F synthetic methods and their application to the preparation of [¹⁸F]-labeled steroids for imaging hormone-responsive cancers. The methods exemplified are fluoride ion displacement of sulfonates and opening of cyclic sulfates, nucleophilic aromatic substitution, and halogen fluoride addition to alkenes.

Original language	English (US)
Pages (from-to)	49-54
Number of pages	6
Journal	Journal of Fluorine Chemistry
Volume	109
Issue number	1
DOIs	https://doi.org/10.1016/S0022-1139(01)00379-7
State	Published - 2001

Keywords

Estrogens
Fluorine-18
Imaging breast tumors
PET
Positron emission tomography
Radiopharmaceuticals

ASJC Scopus subject areas

Biochemistry
Environmental Chemistry
Physical and Theoretical Chemistry
Organic Chemistry
Inorganic Chemistry

Online availability

10.1016/S0022-1139(01)00379-7

Library availability

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Cite this

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title = "Steroids labeled with 18F for imaging tumors by positron emission tomography",

abstract = "The chemistry to label radiopharmaceuticals for imaging with positron emission tomography (PET) with the 2 h half life positron-emitting radionuclide fluorine-18 (18F) requires ease, efficiency, and speed. Furthermore, when high specific activities are needed, as in imaging high affinity, low capacity receptors, reactions need to work well at the tracer level scale. This review covers 18F synthetic methods and their application to the preparation of [18F]-labeled steroids for imaging hormone-responsive cancers. The methods exemplified are fluoride ion displacement of sulfonates and opening of cyclic sulfates, nucleophilic aromatic substitution, and halogen fluoride addition to alkenes.",

keywords = "Estrogens, Fluorine-18, Imaging breast tumors, PET, Positron emission tomography, Radiopharmaceuticals",

author = "Katzenellenbogen, {J. A.}",

note = "Funding Information: We are grateful for the support of our research from the National Institutes of Health and the Department of Energy. I thank many co-workers in my laboratory whose contributions have been highlighted in this brief review, and I am especially thankful to my long-term collaborator, Mike Welch, and his associates at Washington University Medical School, St. Louis.",

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T1 - Steroids labeled with 18F for imaging tumors by positron emission tomography

AU - Katzenellenbogen, J. A.

N1 - Funding Information: We are grateful for the support of our research from the National Institutes of Health and the Department of Energy. I thank many co-workers in my laboratory whose contributions have been highlighted in this brief review, and I am especially thankful to my long-term collaborator, Mike Welch, and his associates at Washington University Medical School, St. Louis.

PY - 2001

Y1 - 2001

N2 - The chemistry to label radiopharmaceuticals for imaging with positron emission tomography (PET) with the 2 h half life positron-emitting radionuclide fluorine-18 (18F) requires ease, efficiency, and speed. Furthermore, when high specific activities are needed, as in imaging high affinity, low capacity receptors, reactions need to work well at the tracer level scale. This review covers 18F synthetic methods and their application to the preparation of [18F]-labeled steroids for imaging hormone-responsive cancers. The methods exemplified are fluoride ion displacement of sulfonates and opening of cyclic sulfates, nucleophilic aromatic substitution, and halogen fluoride addition to alkenes.

AB - The chemistry to label radiopharmaceuticals for imaging with positron emission tomography (PET) with the 2 h half life positron-emitting radionuclide fluorine-18 (18F) requires ease, efficiency, and speed. Furthermore, when high specific activities are needed, as in imaging high affinity, low capacity receptors, reactions need to work well at the tracer level scale. This review covers 18F synthetic methods and their application to the preparation of [18F]-labeled steroids for imaging hormone-responsive cancers. The methods exemplified are fluoride ion displacement of sulfonates and opening of cyclic sulfates, nucleophilic aromatic substitution, and halogen fluoride addition to alkenes.

KW - Estrogens

KW - Fluorine-18

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KW - Positron emission tomography

KW - Radiopharmaceuticals

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