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Labelled compounds of interest as antitumour agents. Part II (1). Synthesis of 2H and 3H isotopomers of RSU 1069 and Ro 03-8799 (pimonidazole)

✍ Scribed by Paul Webb; Michael D. Threadgill

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

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✦ Synopsis

Abstract

^2^H‐ and ^3^H‐Labelled RSU 1069 and Ro 03‐8799 (pimonidazole) have been synthesised by reduction of 1‐(3‐chloro‐2‐oxopropyl)‐2‐nitroimidazole with the appropriately labelled sodium borohydride, followed by ring‐closure of the chlorohydrins and treatment of the resulting epoxides with aziridine or piperidine. In both cases, the specific activities were 200 mCi mmol^−1^ and the radiochemical yields were 86%. The parent compounds are radiosensitisers of hypoxic tumour cells.

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