Synthesis of substituted 5-bromomethyl-4-nitroimidazoles and use for the preparation of the hypoxia-selective multikinase inhibitor SN29966
GL Lu, A Ashoorzadeh, RF Anderson, AV Patterson…
Index: Lu, Guo-Liang; Ashoorzadeh, Amir; Anderson, Robert F.; Patterson, Adam V.; Smaill, Jeff B. Tetrahedron, 2013 , vol. 69, # 43 p. 9130 - 9138
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Abstract
Abstract 5-Bromomethyl-4-nitroimidazoles have utility as bioreductive trigger precursors for the preparation of hypoxia-selective prodrugs. Here we describe an efficient two-step synthesis of 5-(bromomethyl)-1-methyl-4-nitro-1H-imidazole, a preferred precursor, employing an N-bromosuccinimide mediated radical bromination. Use of this precursor to prepare SN29966, a promising hypoxia-selective irreversible pan-ErbB inhibitor is ...
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