Method for production of F-18 labeled amyloid beta ligands

摘要

This invention relates to methods, which provide access to [F-18]fluoropegylated (aryl/heteroaryl vinyl)-phenyl methyl amine derivatives.

主权项

1. A method for producing an injectable formulation of a compound of Formula I suitable for injection into humans comprising the steps of: Step 1: radiolabeling a compound of Formula II with a F-18 fluorinating agent, to obtain a compound of Formula I, if R═H or to obtain compound of Formula III, if R=PG Step 2: if R=PG, cleaving the protecting group PG to obtain a compound of Formula I, and Step 3: purifying and formulating a compound of Formula I wherein:
n=3,X is selected from the group consisting of
a) CH, andb) N,R is selected from the group consisting of
a) H, andb) PG,PG is an amine-protecting group, andLG is a leaving group, wherein Step 3 comprises purifying and formulating a compound of formula I using a HPLC separation using an HPLC solvent eluent consisting of an ethanol/aqueous buffer mixture and wherein the fraction obtained from the HPLC purifying is part of an injectable formulation of a compound of formula I suitable for injection into humans, and wherein the radioactive level of the injectable formulation prepared by the method is more than 50 GBq, wherein the radiochemical purity of the injectable formulation prepared by the method is >95%.