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Syntheses of radiolabeled ABT‐578 for ADME studies
Author(s) -
Rotert G.,
Fan L.,
Shevchenko V. P.,
Nagaev I. Yu.,
Myasoedov N. F.,
Susan A. B.
Publication year - 2006
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.1091
Subject(s) - chemistry , tetrazole , adme , tritium , stereochemistry , biochemistry , in vitro , physics , nuclear physics
Several isotopomers of ABT‐578 ( I , II , III , and IV ) were prepared starting from different labeled precursors: [5'‐ 3 H]‐tetrazole ( 1 ), [5'‐ 14 C]‐tetrazole ( 2 ), [40‐ 3 H]rapamycin ( 3 ), and [2,11,31‐ 3 H]rapamycin ( 4 ). It was shown that the tritium label at the 40 position of rapamycin is lost during an attempted synthesis of [40‐ 3 H]ABT‐578 ( III ). Copyright © 2006 John Wiley & Sons, Ltd.