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Tritium labelling of RAD001—a new rapamycin derivative
Author(s) -
Moenius Th.,
Andres H.,
Acemoglu M.,
Kohler B.,
Schnelli P.,
Zueger C.
Publication year - 2000
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/(sici)1099-1344(200002)43:2<113::aid-jlcr295>3.0.co;2-c
Subject(s) - chemistry , labelling , moiety , tritium , intramolecular force , radiochemistry , lithium (medication) , combinatorial chemistry , stereochemistry , biochemistry , medicine , physics , nuclear physics , endocrinology
RAD001 2 , a new immunosuppressant, was labelled in its hydroxyethyl side chain as well as in the rapamycin skeleton using carrier‐free lithium triethylborotritide and tributyltin tritide (TBTT), respectively. The tritium labelling of the rapamycin moiety followed Curran's strategy of intramolecular hydrogen transfer. Our studies demonstrated that base‐free TBTT is essential for a successful reaction. Copyright © 2000 John Wiley & Sons, Ltd.