Dual-Function Radiosensitizers. α-methyl>-2-nitro-1H-imidazole-1-ethanol and Related Compounds: Preparation via an Aziridine Equivalent

Article abstract of DOI:10.1021/jm00107a047

An improved synthesis of the dual-function radiosensitizer α-<<(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 percent yield.