The first synthesis of [11C]J147, a new potential PET agent for imaging of Alzheimer's disease

  • Bioorg Med Chem Lett. 2013 Jan 15;23(2):524-7. doi: 10.1016/j.bmcl.2012.11.031.
Min Wang  1 ,  Mingzhang Gao ,  Qi-Huang Zheng
Affiliations
  • 1. Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, Room 202, Indianapolis, IN 46202, USA.
PMID: 23237833 DOI: 10.1016/j.bmcl.2012.11.031
Abstract

J147 was synthesized from 2,4-dimethylphenylhydrazine hydrochloride and 3-methoxybenzaldehyde in 2 steps with 71% overall yield. The precursor desmethyl-J147 was synthesized from 3-hydroxybenzaldehyde and 2,4-dimethylphenylhydrazine hydrochloride in 4 steps with 63% overall yield. [(11)C]J147 was prepared from desmethyl-J147 with [(11)C]CH(3)OTf through O-[(11)C]methylation and isolated by HPLC combined with solid-phase extraction (SPE) in 35-50% radiochemical yield based on [(11)C]CO(2) and decay corrected to end of bombardment (EOB), with 370-740 GBq/μmol specific activity at EOB.

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