Purification method

摘要

A diagnostic imaging agent useful for positron emission tomography (PET) imaging as well as to improved hardware for producing such imaging agents is described. Flutemetamol (18F) Injection for the imaging of b amyloid plaques in the brain and methods and devices for preparing same are described including the automated synthesis and purification of [18F]flutemetamol by means of solid phase extraction (SPE).

主权项

1. A purification process comprising the following steps:
(a) passing a diluted crude product reaction mixture comprising [18F]flutemetamol through a first reverse phase solid phase extraction (SPE) cartridge; (b) washing said first reverse phase SPE cartridge with a water/acetonitrile, tetrahydrofuran(THF)/water, methanol(MeOH)/water or isopropanol/water mixture; (c) rinsing said first reverse phase SPE cartridge with water once step (b) is completed; (d) eluting said first reverse phase SPE cartridge with acetonitrile or tetrahydrofuran; (e) directly passing the eluate resulting from said eluting step (d) through a normal phase SPE cartridge to give an acetonitrile or tetrahydrofuran solution comprising purified [18F]flutemetamol; (f) diluting said acetonitrile or tetrahydrofuran solution comprising purified [18F]flutemetamol with water to form a diluted water/acetonitrile or water/tetrahydrofuran solution comprising purified [18F]flutemetamol, wherein said water/acetonitrile or said water/tetrahydrofuran solution contains about 40-70% (v/v) water; (g) passing the diluted water/acetonitrile or said diluted water/tetrahydrofuran solution comprising purified [18F]flutemetamol of step (f) through a second reverse phase SPE cartridge and trapping the [18F]flutemetamol on said second reverse phase SPE cartridge; (h) rinsing said second reverse phase SPE cartridge with water; and (i) eluting the trapped purified [18F]flutemetamol from second reverse phase SPE cartridge with an injectable organic solvent wherein said injectable organic solvent is ethanol or dimethyl sulfoxide (DMSO).