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Synthesis of no-carrier-added and carrier-added YF-labelled haloperidol

Abstract

Fluorine-18 labelled haloperidol ( YF-HP) was synthesized by a fluorine-fluorine exchange reaction on haloperidol, fluorine-chlorine exchange on a chloro-analog of haloperidol, and from YF-labelled p-fluorobenzonitrile prepared by two different exchange reactions. Nucleophilic fluorine was used in the form of tetra n-butylammonium fluoride. The overall radiochemical yield, expressed at the end of syntheses was 5% for exchange in haloperidol and about 2%-3% for exchange in chloroanalog in a 40 min synthesis (from the end of the irradiation). Specific activities up to 1 Ci/mmol for haloperidol and up to 5000 Ci/mmol for chloro-analog as substrates were obtained. The syntheses using p-substituted chloro-and nitro-benzonitriles as starting materials for the exchange reaction gave a product with an average specific activity of about 2000 Ci/mmol and in general an overall radiochemical yield of 5%-10%. Purification of ( YF)haloperidol was done by HPLC on a C-18 column. The radiochemical purity as assessed by thin layer radiochromatography (TLRC) of the final product was at least 95%, with high chemical purity.
Publication Date:
Jul 01, 1985
Product Type:
Journal Article
Reference Number:
AIX-17-012046; EDB-86-043164
Resource Relation:
Journal Name: J. Labelled Compd. Radiopharm.; (United Kingdom); Journal Volume: 22:7; Other Information: Presented in part at the 18. meeting of ACS, St. Louis, MO, USA, April 8-13 1984, and 5. international symposium on radio-pharmaceutical chemistry, Tokyo, Japan, July 9-13 1984
Subject:
38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY; 62 RADIOLOGY AND NUCLEAR MEDICINE; 37 INORGANIC, ORGANIC, PHYSICAL AND ANALYTICAL CHEMISTRY; FLUORINE 18; ISOTOPIC EXCHANGE; RADIOPHARMACEUTICALS; CHEMICAL PREPARATION; IMPURITIES; LABELLING; POSITRON COMPUTED TOMOGRAPHY; BETA DECAY RADIOISOTOPES; BETA-PLUS DECAY RADIOISOTOPES; COMPUTERIZED TOMOGRAPHY; DIAGNOSTIC TECHNIQUES; DRUGS; EMISSION COMPUTED TOMOGRAPHY; FLUORINE ISOTOPES; HOURS LIVING RADIOISOTOPES; ISOTOPES; LABELLED COMPOUNDS; LIGHT NUCLEI; NUCLEI; ODD-ODD NUCLEI; RADIOISOTOPES; SYNTHESIS; TOMOGRAPHY; 400702* - Radiochemistry & Nuclear Chemistry- Properties of Radioactive Materials; 550601 - Medicine- Unsealed Radionuclides in Diagnostics; 400303 - Organic Chemistry- Isotope Exchange & Isotope Separation- (-1987)
OSTI ID:
6302693
Research Organizations:
Montreal Neurological Inst., Quebec, Canada
Country of Origin:
United Kingdom
Language:
English
Other Identifying Numbers:
Journal ID: CODEN: JLCRD
Submitting Site:
HEDB
Size:
Pages: 721-733
Announcement Date:
Jan 01, 1986

Citation Formats

Farrokhzad, S, and Diksic, M. Synthesis of no-carrier-added and carrier-added YF-labelled haloperidol. United Kingdom: N. p., 1985. Web. doi:10.1002/jlcr.2580220713.
Farrokhzad, S, & Diksic, M. Synthesis of no-carrier-added and carrier-added YF-labelled haloperidol. United Kingdom. https://doi.org/10.1002/jlcr.2580220713
Farrokhzad, S, and Diksic, M. 1985. "Synthesis of no-carrier-added and carrier-added YF-labelled haloperidol." United Kingdom. https://doi.org/10.1002/jlcr.2580220713.
@misc{etde_6302693,
title = {Synthesis of no-carrier-added and carrier-added YF-labelled haloperidol}
author = {Farrokhzad, S, and Diksic, M}
abstractNote = {Fluorine-18 labelled haloperidol ( YF-HP) was synthesized by a fluorine-fluorine exchange reaction on haloperidol, fluorine-chlorine exchange on a chloro-analog of haloperidol, and from YF-labelled p-fluorobenzonitrile prepared by two different exchange reactions. Nucleophilic fluorine was used in the form of tetra n-butylammonium fluoride. The overall radiochemical yield, expressed at the end of syntheses was 5% for exchange in haloperidol and about 2%-3% for exchange in chloroanalog in a 40 min synthesis (from the end of the irradiation). Specific activities up to 1 Ci/mmol for haloperidol and up to 5000 Ci/mmol for chloro-analog as substrates were obtained. The syntheses using p-substituted chloro-and nitro-benzonitriles as starting materials for the exchange reaction gave a product with an average specific activity of about 2000 Ci/mmol and in general an overall radiochemical yield of 5%-10%. Purification of ( YF)haloperidol was done by HPLC on a C-18 column. The radiochemical purity as assessed by thin layer radiochromatography (TLRC) of the final product was at least 95%, with high chemical purity.}
doi = {10.1002/jlcr.2580220713}
journal = []
volume = {22:7}
journal type = {AC}
place = {United Kingdom}
year = {1985}
month = {Jul}
}