Synthesis and biological studies of positron-emitting radiopharmaceuticals
Thesis/Dissertation
·
OSTI ID:5629027
The development and clinical evaluation of two-positron emitting radiopharmaceuticals designed to image myelin in humans is reported. Carbon-11-labeled benzyl methyl ether was synthesized by the reaction of carbon-11-labeled methanol and benzyl chloride in dimethyl sulfoxide containing powdered potassium hydroxide in a radiochemical yield of 43% and a synthesis and purification time of 40 minutes. Carbon-11-labeled diphenylmethanol was synthesized by the reaction of carbon-11-labeled carbon dioxide and phenyllithium followed by the reduction of the carbon-11-labeled intermediate to diphenylmethanol via lithium aluminum hydride in a radiochemical yield of 71% and a synthesis and purification time of 38 minutes. Carbon-11-labeled benzyl methyl ether and diphenylmethanol were each evaluated as myelin imaging agents in three patients with multiple sclerosis via positron-emission tomography. In two out of three patients studied with carbon-11-labeled benzyl methyl ether, the distribution of activity in the brain was not consistent with local lipid content. A new synthesis of carbon-11-labeled-DL-phenylalanine labeled in the benzylic position and the synthesis of fluorine-18-labeled 1-(2-nitro-1-imidazolyl)-3-fluoro-2-propanol, a potential in vivo marker of hypoxic tissue, are reported.
- Research Organization:
- Washington Univ., St. Louis, MO (USA)
- OSTI ID:
- 5629027
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
400702* -- Radiochemistry & Nuclear Chemistry-- Properties of Radioactive Materials
550601 -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
BRAIN
CARBON 11
CARBON COMPOUNDS
CARBON DIOXIDE
CARBON ISOTOPES
CARBON OXIDES
CENTRAL NERVOUS SYSTEM
CHALCOGENIDES
CHEMICAL PREPARATION
COMPUTERIZED TOMOGRAPHY
DIAGNOSTIC TECHNIQUES
DIAGNOSTIC USES
DRUGS
EMISSION COMPUTED TOMOGRAPHY
EVEN-ODD NUCLEI
ISOTOPES
LABELLED COMPOUNDS
LIGHT NUCLEI
MINUTES LIVING RADIOISOTOPES
NERVOUS SYSTEM
NUCLEI
ORGANS
OXIDES
OXYGEN COMPOUNDS
POSITRON COMPUTED TOMOGRAPHY
RADIOISOTOPES
RADIOPHARMACEUTICALS
SYNTHESIS
TOMOGRAPHY
USES
400702* -- Radiochemistry & Nuclear Chemistry-- Properties of Radioactive Materials
550601 -- Medicine-- Unsealed Radionuclides in Diagnostics
62 RADIOLOGY AND NUCLEAR MEDICINE
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
BRAIN
CARBON 11
CARBON COMPOUNDS
CARBON DIOXIDE
CARBON ISOTOPES
CARBON OXIDES
CENTRAL NERVOUS SYSTEM
CHALCOGENIDES
CHEMICAL PREPARATION
COMPUTERIZED TOMOGRAPHY
DIAGNOSTIC TECHNIQUES
DIAGNOSTIC USES
DRUGS
EMISSION COMPUTED TOMOGRAPHY
EVEN-ODD NUCLEI
ISOTOPES
LABELLED COMPOUNDS
LIGHT NUCLEI
MINUTES LIVING RADIOISOTOPES
NERVOUS SYSTEM
NUCLEI
ORGANS
OXIDES
OXYGEN COMPOUNDS
POSITRON COMPUTED TOMOGRAPHY
RADIOISOTOPES
RADIOPHARMACEUTICALS
SYNTHESIS
TOMOGRAPHY
USES