DUAL-FUNCTION RADIOSENSITIZERS - ALPHA-[[(2-BROMOETHYL)AMINO]METHYL]-2-NITRO-1H-IMIDAZOLE-1-ETHANOL AND RELATED-COMPOUNDS - PREPARATION VIA AN AZIRIDINE EQUIVALENT

被引：13

作者：

SUTO, MJ

STIER, MA

WERBEL, LM

机构：

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

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 34卷 / 03期

关键词：

D O I：

10.1021/jm00107a047

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

An improved synthesis of the dual-function radiosensitizer alpha-[[2-bromoethyl)amino]methyl]-2-nitro-H-1-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.

引用

页码：1207 / 1209

页数：3

共 13 条

[11]

SEBOLTLEOPOLD JS, UNPUB

[12] NOVEL NITROIMIDAZO[2,1-B]OXAZOLE FORMATION FROM REACTION OF 2,4(5)-DINITROIMIDAZOLE WITH OXIRANES [J].