title: An organotrifluoroborate for broadly applicable one-step 18F-labeling.
abstract: A new zwitterionic organotrifluoroborate is appended to three radiosynthons that afford undergo facile bioconjugation to several clinically relevant peptides and one enzyme inhibitor. Molecularly complex bioconjugates are (18)F-labeled in a single aqueous step in rapid time (<15 min) without HPLC purification to afford tracers in good yields (>200 mCi, 20-40%) at high specific activity (≥3 Ci/μmol) and at >98% purity. PET imaging shows in vivo stability and tumor uptake.
authors.affiliation: Chemistry Department, University of British Columbia, 2036 Main Mall, Vancouver, BC, V6T-1Z1 (Canada).
authors.forename: Zhibo
authors.initials: Z
authors.lastname: Liu
authors.forename: Maral
authors.initials: M
authors.lastname: Pourghiasian
authors.forename: Mark Alex
authors.initials: MA
authors.lastname: Radtke
authors.forename: Joseph
authors.initials: J
authors.lastname: Lau
authors.forename: Jinhe
authors.initials: J
authors.lastname: Pan
authors.forename: Gemma M
authors.initials: GM
authors.lastname: Dias
authors.forename: Donald
authors.initials: D
authors.lastname: Yapp
authors.forename: Kuo-Shyan
authors.initials: KS
authors.lastname: Lin
authors.forename: Francois
authors.initials: F
authors.lastname: Bénard
authors.forename: David M
authors.initials: DM
authors.lastname: Perrin
mesh_terms: D005462:Fluorine Radioisotopes / Q000737:chemistry*; D019788:Fluorodeoxyglucose F18 / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods*
chemical_list: D005462:Fluorine Radioisotopes; D019788:Fluorodeoxyglucose F18
keywords: 18F-labeling; PET imaging; bioconjugation; click chemistry; peptides