Method for synthesizing iodo- or astatoarenes using diaryliodonium salts
AssigneesInstitut National De La Sante Et De La Recherche Medicale (Inserm), Centre National De La Recherche Scientifique, Universite De Nantes, Universite D'Angers, The Government of the United States of America as represented by the Secretary of the Department of Health and Human Services
InventorsFrançois Guerard, Jean-François Gestin, Martin W. Brechbiel, Yong-Sok Lee
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Abstract
The present invention concerns a method of synthesizing a iodo- or astatoarene comprising the reaction of a diaryliodonium compound with a iodide or astatide salt, respectively. The invention also relates to said iodo- or astatoarene and diaryliodonium compound as such. The invention also concerns a method of synthesizing a iodo- or astatolabelled biomolecule and/or vector using said iodo- or astatoarene.
Claims14
A method of synthesizing an astatoarene comprising reacting a diaryliodonium compound with an astatide salt, wherein the diaryliodonium compound is of formula (II):
- wherein:
- Ar1 and Ar2, independently of each other, are chosen from:
- (C6-C10)aryl and heteroaryl groups, said aryl and heteroaryl groups being substituted with one or several substituents selected from:
- (C1-C6)alkyl, (C2-C6)alkynyl, optionally substituted heteroaryl, halogen, NO2, CN, N3, CF3, —ORa, —COORb, —C(O)R8, —N═C═O, —N═C═S, —N(Ra)COORb, —(C1-C6)alkylene-N(Ra)—C(O)—Rb, —(C1-C6)alkylene-N(Ra)—C(O)—(C1-C6)alkylene-Rb, —(C1-C6)alkylene-N(Ra)—C(O)—(C1-C6)alkylene-C(O)O—Rb and maleimidyl, said (C1-C6)alkyl group being optionally substituted with one or several substituents selected from N3, OH, OCH3, CF3, —O—CH2—O—(C1-C6)alkyl, O—(C1-C6)alkenyl and —O—(C1-C6)alkylene-(C6-C10)aryl;
- Ra is H or (C1-C6) alkyl;
- Rb is selected from the group consisting of:
- H, (C1-C6) alkyl, and functional groups able to bind a vector and/or a biomolecule;
- and
- Y is a monovalent anion.
Dependencies are inferred from the claim text.