Concise and Scalable Radiosynthesis of (+)-[¹⁸F]MDL100907 as a Serotonin 5-HT_2A Receptor Antagonist for PET.

ABSTRACT: 5-Hydroxytryptamine (5-HT_2A) receptors play an important role in several psychiatric disorders. In order to investigate the serotonin (5-HT) receptor in vivo, reliable syntheses are required for positron emission tomography (PET) 5-HT radioligands. Owing to the excellent in vivo properties of [¹⁸F]MDL100907 for PET, there has been great interest to develop a novel synthetic route for [¹⁸F]MDL100907. Here, we report a highly efficient, scalable, and expedient synthesis for [¹⁸F]MDL100907. The radiofluorination was performed on a ¹⁸F-labeling boron pinacol ester precursor, which is synthesized using the Liebeskind-Srogl cross-coupling reaction as a key step. Our method is practically more suitable to employ late-stage Cu-me

SUBMITTER: Chavan LN 

PROVIDER: S-EPMC10557077 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature