Citation
T. Moenius et al., Tritium labelling of RAD001 - A new rapamycin derivative, J LABEL C R, 43(2), 2000, pp. 113-120
Citations number
10
Categorie Soggetti
Chemistry & Analysis","Inorganic & Nuclear Chemistry
Journal title
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
ISSN journal
03624803
→ ACNP
Volume
43
Issue
2
Year of publication
2000
Pages
113 - 120
Database
ISI
SICI code
0362-4803(200002)43:2<113:TLOR-A>2.0.ZU;2-M
Abstract
RAD001 (2) under bar, a new immunosuppressant, was labelled in its hydroxye
thyl side chain as well as in the rapamycin skeleton using carrier-free lit
hium triethylborotritide and tributyltin tritide (TBTT), respectively. The
tritium labelling of the rapamycin moiety followed Curran's strategy of int
ramolecular hydrogen transfer. Our studies demonstrated that base-free TBTT
is essential for a successful reaction.