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Dual-function radiosensitizers. Alpha-[[(2-bromoethyl)amino]methyl]-2-nitro-1H-imidazole-1-ethanol and related

M J Suto¹, M A Stier, L M Werbel

¹Parke-Davis Pharmaceutical Research Division, Warner-Lambert Company, Ann Arbor, Michigan 48105.

Journal of Medicinal Chemistry

|March 1, 1991

Abstract:

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.

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