Tritium labelling of RAD001 - A new rapamycin derivative

Article abstract of DOI:10.1002/(SICI)1099-1344(200002)43:2<113::AID-JLCR295>3.0.CO;2-C

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.