Quality Control of 2-Chloro-1,3-bis(2,6-diisopropylphenyl)-1H-imidazol-3-ium chloride. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 2-Chloro-1,3-bis(2,6-diisopropylphenyl)-1H-imidazol-3-ium chloride, is researched, Molecular C27H36Cl2N2, CAS is 1228185-09-8, about HDAC6 Brain Mapping with [18F]Bavarostat Enabled by a Ru-Mediated Deoxyfluorination. Author is Strebl, Martin G.; Campbell, Arthur J.; Zhao, Wen-Ning; Schroeder, Frederick A.; Riley, Misha M.; Chindavong, Peter S.; Morin, Thomas M.; Haggarty, Stephen J.; Wagner, Florence F.; Ritter, Tobias; Hooker, Jacob M..
Histone deacetylase 6 (HDAC6) function and dysregulation have been implicated in the etiol. of certain cancers and more recently in central nervous system (CNS) disorders including Rett syndrome, Alzheimer’s and Parkinson’s diseases, and major depressive disorder. HDAC6-selective inhibitors have therapeutic potential, but in the CNS drug space the development of highly brain penetrant HDAC inhibitors has been a persistent challenge. Moreover, no tool exists to directly characterize HDAC6 and its related biol. in the living human brain. Here, we report a highly brain penetrant HDAC6 inhibitor, Bavarostat, that exhibits excellent HDAC6 selectivity (>80-fold over all other Zn-containing HDAC paralogues), modulates tubulin acetylation selectively over histone acetylation, and has excellent brain penetrance. We further demonstrate that Bavarostat can be radiolabeled with 18F by deoxyfluorination through in situ formation of a ruthenium π-complex of the corresponding phenol precursor: the only method currently suitable for synthesis of [18F]Bavarostat. Finally, by using [18F]Bavarostat in a series of rodent and nonhuman primate imaging experiments, we demonstrate its utility for mapping HDAC6 in the living brain, which sets the stage for first-in-human neurochem. imaging of this important target.
In addition to the literature in the link below, there is a lot of literature about this compound(2-Chloro-1,3-bis(2,6-diisopropylphenyl)-1H-imidazol-3-ium chloride)Quality Control of 2-Chloro-1,3-bis(2,6-diisopropylphenyl)-1H-imidazol-3-ium chloride, illustrating the importance and wide applicability of this compound(1228185-09-8).
Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics