| abstract |
1. The method of radiofluorination, comprising reacting a compound of formula (I) with a compound of formula (II):! ! ! or a compound of formula (III) with a compound of formula (IV)! ! ! where R1 represents an aldehyde moiety, a ketone moiety, a protected aldehyde such as acetal, a protected ketone such as ketal, or a functional group such as a diol or N-terminal serine residue that can be quickly and efficiently oxidized to an aldehyde or ketone with the use of an oxidizing agent; ! R2 is a group selected from primary amine, secondary amine, hydroxylamine, hydrazine, hydrazide, aminoxy, phenylhydrazine, semicarbazide and thiosemicarbazide, and preferably represents a hydrazine, hydrazide or aminoxy group; ! R3 represents a group selected from primary amine, secondary amine, hydroxylamine, hydrazine, hydrazide, aminoxy, phenylhydrazine, semicarbazide or thiosemicarbazide, and preferably represents a hydrazine, hydrazide or aminoxy group; ! R4 is an aldehyde moiety, a ketone moiety, a protected aldehyde such as acetal, a protected ketone such as ketal, or a functional group such as a diol or N-terminal serine residue that can be quickly and efficiently oxidized to an aldehyde or ketone using an oxidizing agent; ! to obtain a conjugate of formula (V) or (VI), respectively:! ! ! where X is —CO — NH—, —NH—, —O—, —NHCONH— or —NHCSNH—, and preferably represents —CO — NH—, —NH— or —O—; Y represents H, alkyl or aryl substituents, and! linker group in the compounds of formulas (II), (IV), (V) and (VI) |