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Issue 9, 2015
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Efficient synthesis of 2-nitroimidazole derivatives and the bioreductive clinical candidate Evofosfamide (TH-302)

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Abstract

Hypoxia, regions of low oxygen, occurs in a range of biological environments, and is involved in human diseases, most notably solid tumours. Exploiting the physiological differences arising from low oxygen conditions provides an opportunity for development of targeted therapies, through the use of bioreductive prodrugs, which are selectively activated in hypoxia. Herein, we describe an improved method for synthesising the most widely used bioreductive group, 2-nitroimidazole. The improved method is applied to an efficient synthesis of the anti-cancer drug Evofosfamide (TH-302), which is currently in Phase III clinical trials for treatment of a range of cancers.

Graphical abstract: Efficient synthesis of 2-nitroimidazole derivatives and the bioreductive clinical candidate Evofosfamide (TH-302)

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Article information


Submitted
02 Jul 2015
Accepted
07 Jul 2015
First published
10 Jul 2015

Org. Chem. Front., 2015,2, 1026-1029
Article type
Research Article
Author version available

Efficient synthesis of 2-nitroimidazole derivatives and the bioreductive clinical candidate Evofosfamide (TH-302)

L. J. O'Connor, C. Cazares-Körner, J. Saha, C. N. G. Evans, M. R. L. Stratford, E. M. Hammond and S. J. Conway, Org. Chem. Front., 2015, 2, 1026
DOI: 10.1039/C5QO00211G

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