RADIOLABELLING METHOD

摘要

The present invention relates to the field of radiopharmaceuticals for in vivo imaging, in particular to a method of labelling a biological targeting molecule with the radioisotope 18F. The invention provides a method of preparation of lyophilised compositions of aminooxy-functionalised biomolecules, as well as radiolabelling methods using the purified materials. Also provided are lyophilised compositions and cassettes comprising such purified compositions. The invention is particularly suitable for use with an automated synthesizer apparatus.

主权项

1. A method of preparation of an aminooxy-functionalised biological targeting molecule lyophilised composition which comprises:
(i) reverse phase chromatographic purification of a protected compound of Formula (IA):
[BTM]-X1   (IA) using a mobile phase, to give purified Compound IA in said mobile phase; (ii) deprotection of the purified Compound IA from step (i), to give a solution of aminooxy compound of Formula (IIA):
[BTM]-O—NH2   (IIA) (iii) lyophilisation of the solution from step (ii), to give a lyophilised composition of said aminooxy compound of Formula (IIA);wherein:
[BTM] is a biological targeting molecule; X1 is a protected aminooxy group of formula: wherein R1 and R2 are independently chosen from C1-3 alkyl, C1-3 fluoroalkyl or C4-6 aryl.