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Tritium‐labelling via an iridium‐based solid‐phase catalyst
Author(s) -
Hickey Michael J.,
Kingston Lee P.,
Lockley William J. S.,
Allen Paul,
Mather Andrew,
Wilkinson David. J.
Publication year - 2007
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1233
Subject(s) - chemistry , catalysis , labelling , iridium , tritium , combinatorial chemistry , organic chemistry , radiochemistry , biochemistry , physics , nuclear physics
A solid‐phase, iridium‐based ortho ‐exchange catalyst has been developed, with the aim of producing cleaner, more efficient, systems for tritium and deuterium labelling. The catalyst, which is a solvated polystyrene‐bound triphenylphosphine complex of cyclooctadienyliridium(I) hexafluorophosphate, was evaluated with respect to more conventional catalysts such as CODIr(PPh 3 ) 2 PF 6 and the Crabtree catalyst using simple model compounds as substrates. Labelling of drug candidate molecules proceeds with high regioselectivity and, after a simple filtration step, affords products with high radiochemical purities directly from the exchange reaction. The solid‐phase catalyst functioned well with a variety of traditional directing groups including nitro, amide, benzophenone and N ‐heterocycles. Copyright © 2007 John Wiley & Sons, Ltd.