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Synthesis of pentamidine labelled with tritium and carbon‐14
Author(s) -
Hesk David,
Jones John R.,
Lockley William J. S.,
Wilkinson David J.
Publication year - 1990
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.2580281111
Subject(s) - chemistry , pentamidine , carbon 14 , tritium , labelling , nucleophilic substitution , radiochemistry , amidine , cyanide , electrophilic substitution , medicinal chemistry , organic chemistry , physics , quantum mechanics , nuclear physics , history , pneumonia , biochemistry , archaeology
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.