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Preparation of tritium‐labelled BIIL 260 of high specific radioactivity
Author(s) -
Shevchenko V.P.,
Nagaev I.Yu.,
Myasoedov N.F.,
Susan A.B.,
Anderskewitz R.,
Birke F.W.,
Switek KH.
Publication year - 2003
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.661
Subject(s) - tritium , chemistry , synthon , radiochemistry , halogenation , tritium illumination , tritiated water , specific activity , chemical synthesis , nuclear chemistry , organic chemistry , nuclear physics , biochemistry , physics , in vitro , enzyme
Various approaches to the synthesis of tritium‐labelled BIIL 260 with high specific radioactivity were investigated. Attempts to incorporate tritium directly into BIIL 260 were made by solid‐phase isotope exchange with tritium gas and by isotope exchange with tritiated water which yielded a final product with specific activities ranging from 2 to 7 Ci/mmol. However, the solid‐phase and liquid‐phase dehalogenations of an appropriate synthon fragment of BIIL 260 followed by its subsequent conversion to the final product via chemical synthesis yielded the desired tritium‐labelled BIIL 260 with specific activities of 25 or 71 Ci/mmol, depending upon the precursors and methods used in the dehalogenation step. Copyright © 2002 John Wiley & Sons, Ltd.