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Synthesis and evaluation of [[sup 18]F]fluoroprogestins and [[sup 18]F]fluorometoprolol

Miscellaneous:

Abstract

The author investigated if specific radioactively labelled compounds could be applied to gain insight into particular psychic diseases, f.e. Parkinson's disease and schizophrenia, by means of Positron Emission Tomography (PET). No appropriate compounds were found. In this thesis the syntheses of fluorine-18 labelled progestins and [beta][sub 1]-adrenergic ligands are described. Three approaches towards [[sup 18]F]fluorination are investigated. The first method concerns direct S[sub N]2-substitution, the second approach is the opening of an epoxide, and the third approach is [[sup 18]F]fluoroalkylation. The positron emitting radionuclide fluorine-18 was used because of its relatively long decay time and the possibility to produce it in high yields and with high specific activity. The target systems which were applied for the production of fluorine-18 are described in chapter two. Important chemical and physical aspects of [[sup 18]F]fluoride are reviewed in the same chapter. In chapter three the synthesis of 21-[[sup 18]F]fluorinated progestins is discussed. The synthesis of four 21-[[sup 18]F]fluoroprogesterone derivatives is described and the results of an in vivo evaluation of two of these ligands are discussed. Possible routes leading to 6[alpha]-[[sup 18]F]fluoroprogestins are presented in chapter four. The radiochemical approaches towards the synthesis of these ligands are discussed. In chapter five the proposed  More>>
Authors:
Publication Date:
May 01, 1993
Product Type:
Miscellaneous
Reference Number:
ECN-93-0E0357; EDB-93-107280
Resource Relation:
Other Information: Proefschrift (Dr.)
Subject:
38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY; 62 RADIOLOGY AND NUCLEAR MEDICINE; FLUORINATED AROMATIC HYDROCARBONS; SYNTHESIS; HEART; ADRENALINE; LABELLED COMPOUNDS; PROGESTERONE; FLUORINE 18; RECEPTORS; LIGANDS; ALKYLATION; EXPERIMENTAL DATA; IN VITRO; IN VIVO; LABELLING; POSITRON COMPUTED TOMOGRAPHY; STEREOCHEMISTRY; ADRENAL HORMONES; AROMATICS; AUTONOMIC NERVOUS SYSTEM AGENTS; BETA DECAY RADIOISOTOPES; BETA-PLUS DECAY RADIOISOTOPES; BODY; CARDIOTONICS; CARDIOVASCULAR AGENTS; CARDIOVASCULAR SYSTEM; CHEMICAL REACTIONS; COMPUTERIZED TOMOGRAPHY; DATA; DIAGNOSTIC TECHNIQUES; DRUGS; EMISSION COMPUTED TOMOGRAPHY; FLUORINE ISOTOPES; HALOGENATED AROMATIC HYDROCARBONS; HORMONES; HOURS LIVING RADIOISOTOPES; INFORMATION; ISOMERIC TRANSITION ISOTOPES; ISOTOPES; KETONES; LIGHT NUCLEI; MEMBRANE PROTEINS; NANOSEC LIVING RADIOISOTOPES; NEUROREGULATORS; NUCLEI; NUMERICAL DATA; ODD-ODD NUCLEI; ORGANIC COMPOUNDS; ORGANIC FLUORINE COMPOUNDS; ORGANIC HALOGEN COMPOUNDS; ORGANS; PREGNANES; PROTEINS; RADIOISOTOPES; STEROID HORMONES; STEROIDS; SYMPATHOMIMETICS; TOMOGRAPHY; 400703* - Radiochemistry & Nuclear Chemistry- Radioisotope Production; 550601 - Medicine- Unsealed Radionuclides in Diagnostics
OSTI ID:
6199385
Research Organizations:
Rijksuniversiteit Groningen (Netherlands)
Country of Origin:
Netherlands
Language:
English
Availability:
Available from Rijksuniversiteit Groningen, Dienst Interne en Externe Betrekkingen, Postbus 72, 9700 AB Groningen (Netherlands)
Submitting Site:
ECN
Size:
Pages: (11 p)
Announcement Date:

Miscellaneous:

Citation Formats

De Groot, T J. Synthesis and evaluation of [[sup 18]F]fluoroprogestins and [[sup 18]F]fluorometoprolol. Netherlands: N. p., 1993. Web.
De Groot, T J. Synthesis and evaluation of [[sup 18]F]fluoroprogestins and [[sup 18]F]fluorometoprolol. Netherlands.
De Groot, T J. 1993. "Synthesis and evaluation of [[sup 18]F]fluoroprogestins and [[sup 18]F]fluorometoprolol." Netherlands.
@misc{etde_6199385,
title = {Synthesis and evaluation of [[sup 18]F]fluoroprogestins and [[sup 18]F]fluorometoprolol}
author = {De Groot, T J}
abstractNote = {The author investigated if specific radioactively labelled compounds could be applied to gain insight into particular psychic diseases, f.e. Parkinson's disease and schizophrenia, by means of Positron Emission Tomography (PET). No appropriate compounds were found. In this thesis the syntheses of fluorine-18 labelled progestins and [beta][sub 1]-adrenergic ligands are described. Three approaches towards [[sup 18]F]fluorination are investigated. The first method concerns direct S[sub N]2-substitution, the second approach is the opening of an epoxide, and the third approach is [[sup 18]F]fluoroalkylation. The positron emitting radionuclide fluorine-18 was used because of its relatively long decay time and the possibility to produce it in high yields and with high specific activity. The target systems which were applied for the production of fluorine-18 are described in chapter two. Important chemical and physical aspects of [[sup 18]F]fluoride are reviewed in the same chapter. In chapter three the synthesis of 21-[[sup 18]F]fluorinated progestins is discussed. The synthesis of four 21-[[sup 18]F]fluoroprogesterone derivatives is described and the results of an in vivo evaluation of two of these ligands are discussed. Possible routes leading to 6[alpha]-[[sup 18]F]fluoroprogestins are presented in chapter four. The radiochemical approaches towards the synthesis of these ligands are discussed. In chapter five the proposed routes to the fluorine-18 labelled [beta][sub 1]-adrenergic ligands are described and evaluated in the synthesis of two model compounds. 1-[[sup 18]F]fluorometoprolol, the [[sup 18]F]fluorinated analogue of a potent beta-blocker, is prepared using one of the investigated methods. The biological effect of fluorine substitution of a [beta][sub 1]-adrenergic ligand is discussed on the basis of an in vitro and in vivo evaluation. 21 figs., 28 schemes, 19 tabs., 182 refs.}
place = {Netherlands}
year = {1993}
month = {May}
}