Literature DB >> 22542014

A new high-yield synthetic route to PET CB1 radioligands [11C]OMAR and its analogs.

Mingzhang Gao1, Min Wang, Qi-Huang Zheng.   

Abstract

OMAR analogs reference standards and their corresponding desmethylated precursors were synthesized from substituted anilines either in 4 and 5 steps with 27-32% and 24-31% yield, or in 3 and 4 steps with 21-30% and 19-28% yield, respectively. [(11)C]OMAR and its analog radioligands were prepared from their desmethylated precursors with [(11)C]CH(3)OTf through O-[(11)C]methylation and isolated by HPLC combined with solid-phase extraction (SPE) in 50-65% radiochemical yields 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.

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Year:  2012        PMID: 22542014     DOI: 10.1016/j.bmcl.2012.04.030

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


  4 in total

1.  In vivo SPECT and ex vivo autoradiographic brain imaging of the novel selective CB1 receptor antagonist radioligand [125I]SD7015 in CB1 knock-out and wildtype mouse.

Authors:  Domokos Máthé; Ildikó Horváth; Krisztián Szigeti; Sean R Donohue; Victor W Pike; Zisheng Jia; Catherine Ledent; Miklós Palkovits; Tamás F Freund; Christer Halldin; Balázs Gulyás
Journal:  Brain Res Bull       Date:  2013-01-11       Impact factor: 4.077

2.  Copper triflate-mediated synthesis of 1,3,5-triarylpyrazoles in [bmim][PF6] ionic liquid and evaluation of their anticancer activities.

Authors:  V Kameshwara Rao; Rakesh Tiwari; Bhupender S Chhikara; Amir Nasrolahi Shirazi; Keykavous Parang; Anil Kumar
Journal:  RSC Adv       Date:  2013-09-21       Impact factor: 3.361

Review 3.  Is There a Role for GPCR Agonist Radiotracers in PET Neuroimaging?

Authors:  Matthieu Colom; Benjamin Vidal; Luc Zimmer
Journal:  Front Mol Neurosci       Date:  2019-10-18       Impact factor: 5.639

4.  Nitrileimines as an alternative to azides in base-mediated click [3 + 2] cycloaddition with methylene active nitriles.

Authors:  Mykola A Tupychak; Olga Ya Shyyka; Nazariy T Pokhodylo; Mykola D Obushak
Journal:  RSC Adv       Date:  2020-04-03       Impact factor: 4.036

  4 in total

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