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Synthesis of pentamidine labelled with tritium and carbon-14

✍ Scribed by David Hesk; John R. Jones; William J. S. Lockley; David J. Wilkinson

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

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✦ Synopsis

Abstract

Tritium labelled pentamidine has been prepared with a specific activity of 90 mCi mmol^−1^ using a one‐step exchange reaction between the unlabelled drug and tritiated water. The labelling utilised a homogeneous rhodium trichloride catalyst and yielded pentamidine regiospecifically labelled in the positions ortho to the amidine groups. Carbon‐14 labelled pentamidine was prepared via a seven‐step procedure in which the isotope was introduced via a nucleophilic substitution of 4‐bromo‐phenol with copper(I) [^14^C]cyanide.

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