Dual-function radiosensitizers.. alpha.-[[(2-Bromoethyl) amino] methyl]-2-nitro-1H-imidazole-1-ethanol and related compounds: preparation via an aziridine equivalent

MJ Suto, MA Stier, LM Werbel

Index: Suto, Mark J.; Stier, Michael A.; Werbel, Leslie M. Journal of Medicinal Chemistry, 1991 , vol. 34, # 3 p. 1207 - 1209

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Citation Number: 11

Abstract

Conclusion In conclusion, we have synthesized 2 in 47% yield overall, in two steps from 2- nitroimidazole. The synthesis does not use 1 as an intermediate nor does it use the highly toxic ethylenimine and thus eliminates the remaining hurdle preventing the further clinical development of 2. We have also shown that 2 can be cleanly converted to 1 in situ. In addition, this work has resulted in the synthesis of a number of desoxy analogues of 2 ( ...