Total synthesis and evaluation of [18F]MHMZ

Bioorganic & Medicinal Chemistry Letters
Matthias M HerthF Rösch

Abstract

Radiochemical labeling of MDL 105725 using the secondary labeling precursor 2-[(18)F]fluoroethyltosylate ([(18)F]FETos) was carried out in yields of approximately 90% synthesizing [(18)F]MHMZ in a specific activity of approximately 50MBq/nmol with a starting activity of approximately 3GBq. Overall radiochemical yield including [(18)F]FETos synthon synthesis, [(18)F]fluoroalkylation and preparing the injectable [(18)F]MHMZ solution was 42% within a synthesis time of approximately 100 min. The novel compound showed excellent specific binding to the 5-HT(2A) receptor (K(i)=9.0 nM) in vitro and promising in vivo characteristics.

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Citations

Jun 16, 2011·Medicinal Research Reviews·Louise M PatersonGitte M Knudsen
Jul 20, 2010·Chemical Biology & Drug Design·Vasko KramerFrank Rösch
Dec 30, 2014·Bioorganic & Medicinal Chemistry·Hanno SchiefersteinFrank Rösch
Feb 7, 2015·Bioorganic & Medicinal Chemistry Letters·Valdemar L AndersenJesper L Kristensen
Feb 10, 2011·Neuropsychobiology·Ulrich SchmittFabian Debus
Sep 1, 2017·Journal of Labelled Compounds & Radiopharmaceuticals·Fraser Graeme EdgarMatthias M Herth
May 23, 2015·Journal of Labelled Compounds & Radiopharmaceuticals·Matthias M Herth, Gitte M Knudsen
Oct 14, 2019·European Journal of Nuclear Medicine and Molecular Imaging·Vasko KramerMatthias M Herth
Oct 20, 2020·EJNMMI Research·Vladimir ShalgunovMatthias M Herth
Nov 2, 2019·Neuropharmacology·Elina T L'EstradeMatthias M Herth

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