Literature DB >> 24309505

Concise and high-yield synthesis of T808 and T808P for radiosynthesis of [(18)F]-T808, a PET tau tracer for Alzheimer's disease.

Mingzhang Gao1, Min Wang1, Qi-Huang Zheng2.   

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).
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Alzheimer’s disease (AD); Automation; Positron emission tomography (PET); Tau tracer; [(18)F]-T808

Mesh:

Substances:

Year:  2013        PMID: 24309505     DOI: 10.1016/j.bmcl.2013.11.025

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

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