Journal of Medicinal Chemistry p. 1207 - 1209 (1991)
Update date:2022-08-04
Topics:
Suto, Mark J.
Stier, Michael A.
Werbel, Leslie M.
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.
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