Synthesis and biological studies of positron-emitting radiopharmaceuticals
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
- Resource Relation:
- Other Information: Thesis (Ph. D.)
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
62 RADIOLOGY AND NUCLEAR MEDICINE
BRAIN
POSITRON COMPUTED TOMOGRAPHY
RADIOPHARMACEUTICALS
CHEMICAL PREPARATION
CARBON 11
CARBON DIOXIDE
DIAGNOSTIC USES
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BODY
CARBON COMPOUNDS
CARBON ISOTOPES
CARBON OXIDES
CENTRAL NERVOUS SYSTEM
CHALCOGENIDES
COMPUTERIZED TOMOGRAPHY
DIAGNOSTIC TECHNIQUES
DRUGS
EMISSION COMPUTED TOMOGRAPHY
EVEN-ODD NUCLEI
ISOTOPES
LABELLED COMPOUNDS
LIGHT NUCLEI
MINUTES LIVING RADIOISOTOPES
NERVOUS SYSTEM
NUCLEI
ORGANS
OXIDES
OXYGEN COMPOUNDS
RADIOISOTOPES
SYNTHESIS
TOMOGRAPHY
USES
400702* - Radiochemistry & Nuclear Chemistry- Properties of Radioactive Materials
550601 - Medicine- Unsealed Radionuclides in Diagnostics