Manual and automated Cu-mediated radiosynthesis of the PARP inhibitor [18F]olaparib was written by Guibbal, Florian;Isenegger, Patrick G.;Wilson, Thomas C.;Pacelli, Anna;Mahaut, Damien;Sap, Jeroen B. I.;Taylor, Nicholas J.;Verhoog, Stefan;Preshlock, Sean;Hueting, Rebekka;Cornelissen, Bart;Gouverneur, Veronique. And the article was included in Nature Protocols in 2020.Category: pyridazine This article mentions the following:
Abstract: PET is a diagnostic nuclear imaging modality that relies on automated protocols to prepare agents labeled with a positron-emitting radionuclide (e.g., 18F). In recent years, new reactions have appeared for the 18F-labeling of agents that are difficult to access by applying traditional radiochem., for example those requiring 18F incorporation into unactivated (hetero)arenes. However, automation of these new methods for translation to the clinic has progressed slowly because extensive modification of manual protocols is typically required when implementing novel 18F-labeling methodologies within automated modules. Here, we describe the workflow that led to the automated radiosynthesis of the poly(ADP-ribose) polymerase (PARP) inhibitor [18F]olaparib. First, we established a robust manual protocol to prepare [18F]olaparib from the protected N-[2-(trimethylsilyl)ethoxy]methyl (SEM) arylboronate ester precursor in a 17% ± 5% (n = 15; synthesis time, 135 min) non-decay-corrected (NDC) activity yield, with molar activity (Am) up to 34.6 GBq/μmol. Automation of the process, consisting of copper-mediated 18F-fluorodeboronation followed by deprotection, was achieved on an Eckert & Ziegler Modular-Lab radiosynthesis platform, affording [18F]olaparib in a 6% ± 5% (n = 3; synthesis time, 120 min) NDC activity yield with Am up to 319 GBq/μmol. In the experiment, the researchers used many compounds, for example, Imidazo[1,2-b]pyridazine (cas: 766-55-2Category: pyridazine).
Imidazo[1,2-b]pyridazine (cas: 766-55-2) belongs to pyridazine derivatives. The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Specifically, the pyridazine moiety is an important structural feature of various pharmacologically important compounds with activities like antimicrobial, analgesic, anti-inflammatory, antiplatelet, anticancer, antisecretory, antiulcer, antidepressant, cardiotonic, vasodilator, antiarrhythmic, and hypocholesterolaemic.Category: pyridazine
Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem