1255762-99-2Relevant academic research and scientific papers
PREPARATION OF LABELLED COMPOUNDS
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Page/Page column 101-102, (2010/12/18)
The invention relates to a process for producing a labelled compound, which process comprises treating a compound of formula (I), wherein X is a moiety to be labelled or a detectable label, and R1, R2, R3 and R4 are substitutent groups as defined herein; with a compound of formula (II) : N3-L-Y (π) wherein Y is a detectable label or a moiety to be labelled, provided that if X in the compound of formula (I) is a moiety to be labelled, then Y is a detectable label and if X in the compound of formula (I) is a detectable label, then Y is a moiety to be labelled; and L is a bond or a linking group, thereby producing a labelled compound of formula (IH) by Staudinger Ligation. Groups R3 and R4 may comprise fluorous moieties, in order to facilitate purification of the labelled compound of formula (IH). The invention also provides methods of imaging a human or non-human patient or a cell or in vitro sample, using the labelled compound of formula (III) thus produced, as well as imaging methods in which the compounds of formulae (I) and (II) are administered to the patient, cell or sample. The invention further provides novel compounds of formula (I) and formula (III), a process for producing the compounds of formula (T), and a combination product for medical imaging comprising a compound of formula (I) and a compound of formula (II).
