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U.S. Department of Energy
Office of Scientific and Technical Information
 

(Development of radionuclides from the LAMPF facility)

Technical Report ·
DOI:https://doi.org/10.2172/6545214· OSTI ID:6545214
;
The research objectives and goals of 1983--84 to date include further investigation of 1-halogenated and B-/C-ring halogenated and radio halogenated estradiol derivatives for potential use as receptor-binding radiopharmaceuticals. Our group has devised synthetic routes to 1-bromo, 1-chloro- and 1-fluoroestradiol via electrophilic halogenation of the aromatic A-ring. Work is presently underway to prepare the 1-iodo derivative using a similar methodology. The 11 {beta}-methoxy, 17 {alpha}-ethynyl and 11 {beta}-methoxy-17 {alpha}-ethynyl derivatives are of synthetic interest if the in vitro binding affinities of the parent compounds are favorable. The B- and C-ring vinyl halides' which were proposed in the current contract could not be prepared using the hydrazone intermediates described. Presently, other methods which show promise are being investigated. Stable B-ring brominated derivatives of estradiol have been prepared by our group. Their in vitro properties are currently under investigation. 15 refs.
Research Organization:
New Mexico Univ., Albuquerque, NM (USA). School of Medicine
Sponsoring Organization:
DOE/ER
DOE Contract Number:
AS04-81EV10596
OSTI ID:
6545214
Report Number(s):
DOE/EV/10596-T4; ON: DE91000115
Country of Publication:
United States
Language:
English

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Related Subjects

38 RADIATION CHEMISTRY, RADIOCHEMISTRY, AND NUCLEAR CHEMISTRY
400703* -- Radiochemistry & Nuclear Chemistry-- Radioisotope Production
550201 -- Biochemistry-- Tracer Techniques
550604 -- Medicine-- Unsealed Radionuclides in Therapy-- (1980-)
59 BASIC BIOLOGICAL SCIENCES
62 RADIOLOGY AND NUCLEAR MEDICINE
AFFINITY
BETA DECAY RADIOISOTOPES
BETA-PLUS DECAY RADIOISOTOPES
BROMINATION
BROMINE 77
BROMINE ISOTOPES
CHEMICAL REACTIONS
DAYS LIVING RADIOISOTOPES
DEAMINATION
DISEASES
DOCUMENT TYPES
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ESTRADIOL
ESTRANES
ESTROGENS
HALIDES
HALOGEN COMPOUNDS
HALOGENATION
HORMONES
HYDRAZONES
HYDROXY COMPOUNDS
IN VITRO
INTERMEDIATE MASS NUCLEI
ISOTOPES
LABELLED COMPOUNDS
LABELLING
MEDICINE
MINUTES LIVING RADIOISOTOPES
NEOPLASMS
NUCLEAR MEDICINE
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
PROGRESS REPORT
RADIOISOTOPES
RADIOLOGY
RADIOPHARMACEUTICALS
RADIOTHERAPY
STEROID HORMONES
STEROIDS
SYNTHESIS
THERAPEUTIC USES
THERAPY
USES