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Labelled compounds of interest as antitumour agents. Part III (1). Synthesis of 2H and 3H isotopomers of etanidazole (SR 2508)

✍ Scribed by Paul Webb; Michael D. Threadgill

Publisher
John Wiley and Sons
Year
1990
Tongue
French
Weight
265 KB
Volume
28
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Chemically and radiochemically efficient syntheses of N‐(2‐hydroxy‐2‐[^2^H]ethyl)‐2‐(2‐nitroimidazol‐l‐yl)acetamide and N‐(2‐hydroxy‐2‐[^3^H]ethyl)‐2‐(2‐nitroimidazol‐1‐yl)acetamide, isotopomers of the hypoxic cell radiosensitiser etanidazole (SR 2508), have been achieved by reduction of the corresponding aldehyde with isotopically labelled sodium borohydride. The primary kinetic deuterium isotope effect for the process is 1.5.

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