[EN] SUBSTITUTED ARYL-FLUOROBORATES AS IMAGING AGENTS<br/>[FR] ARYL-FLUOROBORATES SUBSTITUÉS EN TANT QU'AGENTS D'IMAGERIE
申请人:UNIV BRITISH COLUMBIA
公开号:WO2009012596A1
公开(公告)日:2009-01-29
Substituted aryl-boron compounds comprising at least one 18F atom, as illustrated by the formula (I), where at least one of Y1 or Y2 is 18F and A1 is a substituted aromatic ring, with G1-5 being, independently, C or N, and where the substitutents of the aromatic ring or polycyclic moiety (other than boron) comprise at least one electron-withdrawing group (EWG), providing that sigma total (σ total) for all substituents on the aromatic ring or polycyclic moiety except B is about 0.06 or more when said at least one EWG is positioned ortho to B, or about 0.2 or more when no EWG is positioned ortho to B. The compounds include neutral (N=1) and ionic borate (N=2) embodiments. The compounds are useful as positron emission tomography (PET) imaging agents.
含有至少一个18F原子的取代芳基硼化合物,如公式(I)所示,其中Y1或Y2中至少有一个是18F,A1为取代芳香环,其中G1-5独立地为C或N,芳香环或多环基团(除硼外)的取代基包括至少一个电子吸引基(EWG),前提是当至少一个EWG位于B的正交位置时,芳香环或多环基团的所有取代基的总σ(σ total)约为0.06或更高,或当没有EWG位于B的正交位置时,约为0.2或更高。该化合物包括中性(N = 1)和离子硼酸酯(N = 2)实施例。该化合物可用作正电子发射断层扫描(PET)成像剂。