Solid-phase fluorination of uracil and cytosine

摘要

The invention relates to a process for the production of an 18F-labelled tracer which comprises treatment of a solid support-bound precursor of formula (I): SOLID SUPPORT-LINKER-I+-TRACER (I) Y- wherein the TRACER is of formula (A): or an amine protected derivative thereof, wherein Y- is an anion, preferably trifluoromethylsulphonate (triflate) anion; and R1 is either (i) a group CH-NP1AP2A in which P1A and P2A are each independently hydrogen or a protecting group, or (ii) a carbonyl group; with 18F- to produce the labelled tracer of formula (II) or an amine protected derivative thereof, wherein R1 is as defined for the compound of formula (I).