Bioorganic & Medicinal Chemistry Letters 2013-01-15

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

Min Wang, Mingzhang Gao, Qi-Huang Zheng

文献索引：Bioorg. Med. Chem. Lett. 23(2) , 524-7, (2013)

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摘要

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.Copyright © 2012 Elsevier Ltd. All rights reserved.