NEW NUCLEOPHILE-REACTIVE SULFONATED COMPOUNDS FOR THE (RADIO)LABELLING OF (BIO)MOLECULES; PRECURSORS AND CONJUGATES THEREOF

摘要

The invention relates to nucleophile-reactive sulfonated compounds used as precursors to (radio)labelled (bio)molecules suitable mainly for medical applications. The aim of the invention is to provide novel prosthetic compounds or groups, the synthesis of which is straightforward, easy and automatable, enabling access to economical and effective, (radio)labelled, complex and fragile - especially water-soluble and more especially amine-containing- (bio)molecules. The aim is achieved by the invention, which involves precursors and compounds of respective formulae (Ip), (I). Said nucleophile-reactive sulfonated compounds are produced by pre-introduction of a nucleophilic compound R*, e.g. Fluorine- 18, through an unusal nucleophile-induced ring-opening reaction of the sultone (e.g. 1,3-propanesultone) moiety of the precursor. The invention also relates to the methods for producing the abovementioned precursors and compounds, as well as for the conjugation of these compounds with (bio)molecules, and to the drugs obtained through this method.