Dual-function radiosensitizers. Alpha-(((2-bromoethyl)amino)methyl)-2-nitro-1H-imidazole-1-ethanol and related compounds: Preparation via an aziridine equivalent
Journal Article
·
· Journal of Medicinal Chemistry; (USA)
- Warner-Lambert Company, Ann Arbor, MI (USA)
An improved synthesis of the dual-function radiosensitizer alpha-(((2-bromoethyl)amino)methyl)-2-nitro-1H-imidazole-1-ethanol (2, RB 6145) has been developed. Previously, the synthetic difficulties associated with this compound limited its attractiveness as a clinical candidate, although its radiosensitizing activity in preclinical models warranted its further development. The synthesis described uses a 2-oxazolidinone as an aziridine equivalent and provides 2 in 47% yield.
- OSTI ID:
- 5924708
- Journal Information:
- Journal of Medicinal Chemistry; (USA), Journal Name: Journal of Medicinal Chemistry; (USA) Vol. 34:3; ISSN JMCMA; ISSN 0022-2623
- Country of Publication:
- United States
- Language:
- English
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OSTI ID:6509587
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OSTI ID:6167404
Related Subjects
550603 -- Medicine-- External Radiation in Therapy-- (1980-)
560151* -- Radiation Effects on Animals-- Man
62 RADIOLOGY AND NUCLEAR MEDICINE
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
CHEMICAL PREPARATION
CHEMICAL REACTIONS
DRUGS
ESTERIFICATION
MOLECULAR STRUCTURE
RADIOSENSITIVITY EFFECTS
RADIOSENSITIZERS
SYNTHESIS
560151* -- Radiation Effects on Animals-- Man
62 RADIOLOGY AND NUCLEAR MEDICINE
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
CHEMICAL PREPARATION
CHEMICAL REACTIONS
DRUGS
ESTERIFICATION
MOLECULAR STRUCTURE
RADIOSENSITIVITY EFFECTS
RADIOSENSITIZERS
SYNTHESIS