Document Detail

Synthesis of new hypoxia markers EF1 and [18F]-EF1.
MedLine Citation:
PMID:  10581679     Owner:  NLM     Status:  MEDLINE    
We report on the preparation of a hypoxia marker 2-(2-nitroimidazol-1[H]-yl)-N-(3-fluoropropyl)acetamide (EF1) and its 18F analog, 2-(2-nitroimidazol-1[H]-yl)-N- (3-[18F]fluoropropyl)acetamide ([18F]-EF1). Two methods for the preparation of 3-fluoropropylamine, the EF1 side chain, are described. [18F]-EF1 was prepared with a radiochemical yield of 2% by nucleophilic substitution of bromine in 2-(2-nitroimidazol-1[H]-yl)-N-(3-bromopropyl)acetamide (EBr1) by carrier-added 18F in DMSO at 120 degrees C. Our results demonstrate the preparation of clinically relevant amounts of [18F]-EF1 for use as a non-invasive hypoxia marker with detection using positron emission tomography (PET).
A V Kachur; W R Dolbier; S M Evans; C Y Shiue; G G Shiue; K A Skov; I R Baird; B R James; A R Li; A Roche; C J Koch
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine     Volume:  51     ISSN:  0969-8043     ISO Abbreviation:  Appl Radiat Isot     Publication Date:  1999 Dec 
Date Detail:
Created Date:  2000-01-11     Completed Date:  2000-01-11     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9306253     Medline TA:  Appl Radiat Isot     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  643-50     Citation Subset:  IM    
Department of Radiation Oncology, University of Pennsylvania, Philadelphia 19104, USA.
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MeSH Terms
Anoxia / diagnosis*,  metabolism
Biological Markers / analysis
Fluorine Radioisotopes / chemistry
Isotope Labeling / methods
Nitroimidazoles / chemical synthesis*
Radiopharmaceuticals / chemical synthesis*
Tomography, Emission-Computed
Reg. No./Substance:
0/2-(2-nitroimidazol-1H-yl)-N-(3-fluoropropyl)acetamide; 0/Biological Markers; 0/Fluorine Radioisotopes; 0/Nitroimidazoles; 0/Radiopharmaceuticals

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