title: Concise and high-yield synthesis of T808 and T808P for radiosynthesis of [(18)F]-T808, a PET tau tracer for Alzheimer's disease.
abstract: The authentic standard T808 and its corresponding mesylate precursor T808P were synthesized in six steps using ethyl vinyl ether and trichlorocetyl chloride as starting materials. The overall chemical yields of T808 and T808P were 35% and 52%, respectively. [(18)F]-T808 was synthesized from T808P by the nucleophilic substitution with K[(18)F]F/Kryptofix 2.2.2 and isolated by HPLC combined with solid-phase extraction (SPE) purification in 35-45% radiochemical yield with 37-370GBq/μmol specific activity at end of bombardment (EOB).
authors.affiliation: Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, Room 202, Indianapolis, IN 46202, USA.
authors.forename: Mingzhang
authors.initials: M
authors.lastname: Gao
authors.affiliation: Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, Room 202, Indianapolis, IN 46202, USA.
authors.forename: Min
authors.initials: M
authors.lastname: Wang
authors.affiliation: Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, Room 202, Indianapolis, IN 46202, USA. Electronic address: qzheng@iupui.edu.
authors.forename: Qi-Huang
authors.initials: QH
authors.lastname: Zheng
mesh_terms: D000544:Alzheimer Disease / Q000175:diagnosis* / Q000378:metabolism*; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry; D005462:Fluorine Radioisotopes / Q000737:chemistry; D006801:Humans; D015394:Molecular Structure; D049268:Positron-Emission Tomography; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry; D016875:tau Proteins / Q000032:analysis* / Q000378:metabolism
chemical_list: D001562:Benzimidazoles; D005462:Fluorine Radioisotopes; D011743:Pyrimidines; C000588468:T808 compound; D016875:tau Proteins
keywords: Alzheimer’s disease (AD); Automation; Positron emission tomography (PET); Tau tracer; [(18)F]-T808