18F-labeled precursor of PET radioactive medical supplies, and preparation method thereof

摘要

The present invention relates to a precursor of positron emission tomography (PET) radioactive medical supplies, a preparation method thereof, and an application thereof, and more specifically, to a precursor having a tetravalent organic salt leaving group, a preparation method, and a method for preparing desired PET radioactive medical supplies in a high radiochemical yield within a short preparation time by introducing 18F using the same through a single step. The precursor having a tetravalent organic salt leaving group of the present invention can simplify the known complex multistep preparation of radioactive medical supplies into a single step, can save production costs because an excessive amount of a phase transfer catalyst is not required, facilitates separation of a compound after reaction, and enables rapid reaction velocity. The features are appropriate for the mass production of PET radioactive medical supplies by an automated synthesis system.

主权项

1. A precursor for the preparation of F-18 labeled radiopharmaceuticals represented by the following Chemical Formula 1: wherein, in Chemical Formula 1, R1 is a part excluding a —X—CH2—18F part from an 18F-labeled radiotracer and represents a C1-C1000 hydrocarbon group in which a carbon in the main chain of the C1-C1000 hydrocarbon group may be non-replaced or replaced by an oxygen, a nitrogen, a sulfur, a phosphorus or combinations thereof and a hydrogen in the main chain may be non-replaced or replaced by a halogen, X represents an oxygen, and the leaving group is a salt consisting of (i) a tetravalent cation and (ii) an anion of Y, and the salt represents wherein one nitrogen within the ring of the tetravalent cation is substituted with R3, and each carbon within the ring of the tetravalent cation may be independently non-substituted or substituted with R2, respectively, R2 and R3 are independently a C1-C20 hydrocarbon group in which a carbon in the main chain of the C1-C20 hydrocarbon group may be non-replaced or replaced by an oxygen, a nitrogen, a sulfur or combinations thereof, and a hydrogen in the main chain may be non-replaced or replaced by a halogen, and Y is selected from the group consisting of trifluoromethanesulfonate (CF3SO3−), paratoluenesulfonate, methanesulfonate and paranitrobenzenesulfonate.