Synthesis of [18F]-N-succinimidyl 4-(fluoromethyl)benzoate from N-succinimidyl-4-[(4-nitrobenzenesulfonyl)oixylmethyl]benzoate
Creators
- 1. National Institute of Health, Bethesda, MD (United States)
Description
High specific [18F]-N-succinimidyl 4-(fluoromethyl)benzoate has been prepared from N-succinimidyl-4-[(4-nitrobenzenesulfonyl)oxymethyl]benzoate in one chemical step. The reaction was carried out in acetone at room temperature for 5 minutes using Kryptofix 2.2.2/18F-. Overall yields for the synthesis were between 13% and 18% (EOS) in 45-50 minutes, including HPLC purification. The specific activity was about 1900 Ci/mmol (EOB). About 150 μg of proteins, such as rabbit anti HSA antibody and transferrin, have been labeled with 60-70% labeling efficiency in 10 minutes. The biodistribution (% ID/g) in rats (3/group) showed that the labeled antibody was stable in vivo (1.5 hr): blood (5.5), liver (1,4), spleen (1.9), kidney (1.0), bone (0.7) and urine (2.9, 3 hr). No significant increase of defluorination was observed 3 hours after injection. About 20 μg of erythropoietin was also successfully labeled with about 25% labeling efficiency
Additional details
Publishing Information
- Publisher
- American Chemical Society.
- Imprint Place
- Washington, DC (United States)
- Imprint Title
- 208th ACS national meeting
- Imprint Pagination
- 2072 p.
- Journal Page Range
- p. 1071, Paper NUCL 27.
Conference
- Title
- 208. American Chemical Society national meeting.
- Dates
- 21-26 Aug 1994.
- Place
- Washington, DC (United States).
INIS
- Country of Publication
- United States
- Country of Input or Organization
- United States
- INIS RN
- 26019629
- Subject category
- S38: RADIATION CHEMISTRY, RADIOCHEMISTRY AND NUCLEAR CHEMISTRY; S63: RADIATION, THERMAL, AND OTHER ENVIRONMENTAL POLLUTANT EFFECTS ON LIVING ORGANISMS AND BIOLOGICAL MATERIALS;
- Resource subtype / Literary indicator
- Conference
- Descriptors DEI
- ANTIBODIES; CHEMICAL PREPARATION; ERYTHROPOIETIN; FLUORINE 18; LABELLING; RADIOPHARMACEUTICALS; TISSUE DISTRIBUTION; TRANSFERRIN
- Descriptors DEC
- BETA DECAY RADIOISOTOPES; BETA-PLUS DECAY RADIOISOTOPES; DISTRIBUTION; DRUGS; FLUORINE ISOTOPES; GLOBULINS; GLOBULINS-BETA; HOURS LIVING RADIOISOTOPES; ISOMERIC TRANSITION ISOTOPES; ISOTOPES; LABELLED COMPOUNDS; LIGHT NUCLEI; MATERIALS; METALLOPROTEINS; NANOSEC LIVING RADIOISOTOPES; NUCLEI; ODD-ODD NUCLEI; ORGANIC COMPOUNDS; PROTEINS; RADIOACTIVE MATERIALS; RADIOISOTOPES; SYNTHESIS
Optional Information
- Secondary number(s)
- CONF-940813--.