
Journal of labelled compounds and radiopharmaceuticals p. 113 - 120 (2000)
Update date:2022-08-04
Topics:
Moenius
Andres
Acemoglu
Kohler
Schnelli
Zueger
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.
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(2003)