Process for the manufacture of an 18F-labelled glycosylation reagent as well as 18F-glycosylation reagent and its use

摘要

An <18>F-labelled glycosylating agent is prepared by: (a) reaction of a hexose (I) with phosphoric acid (H3PO4); (b) hydrolysis of the product with a base; and (c) reaction of the product with uridine triphosphate (UTP) in the presence of pyrophosphorylase and Mg<2+>. Preparation of an <18>F-labelled glycosylating agent comprises: (a) reaction of a hexose of formula (I) with phosphoric acid (H3PO4); (b) hydrolysis of the product with a base; and (c) reaction of the product with uridine triphosphate (UTP) in the presence of a phosphorylase and Mg<2+>. one group R = <18>F in position 2, 3, 4 or 6 of the hexose ring, and the other three = a protecting group which is linked to the hexose ring via an oxygen atom An Independent claim is included for a glycosylating reagent of formula (II): one group R' = <18>F in position 2, 3, 4 or 6 of the hexose ring, and the other three R' groups = OH; OUDP = a uridine diphosphate group