The current role of PET/CT in urological malignancies

Lima, Mariana; Camacho, Mariana; Carvalheira, José Barreto Campello; Biggi, Aline; Lima, Marcelo Lopes de; Ciampi, Juliana; Salis, F.V.; Silveira, Marina Bicalho; Ferreira, Ubirajara; Etchebehere, Elba

doi:10.1007/s40336-020-00378-w

Cited by 3 publications

(1 citation statement)

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“…At the same time, the half-life of 68 Ga is adequately short to prevent long-term radiation exposure of patients and personnel [6,10]. By now a wide range of specifically designed bifunctional ligands are available, making an equally broad spectrum of 68 Ga radiopharmaceuticals with different fields of application accessible [10][11][12]. Our group has designed and established the 68 Ga chelator group TAoS-DAZA as a potential hepatobiliary PET imaging agent [1,13].…”

Section: Introductionmentioning

confidence: 99%

The synthesis of N ,1,4-tri(alkoxy-hydroxybenzyl)-1,4-diazepane-amines: investigations on reaction characteristics and mechanism

Zenner,

Steinmetzer,

Ueberschaar

et al. 2024

R. Soc. Open Sci.

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1,4-Diazepane-6-amine (DAZA) can be alkylated with three 2-hydroxybenzyl pendant arms, resulting in hexadentate chelators suitable for coordination of radiometals like 68 Ga. These chelators, N ,1,4-tri(alkoxy-2-hydroxybenzyl)-DAZA, can be produced via a one-pot synthesis, with the first step being a carbonyl amine condensation of DAZA with two respective 4-alkoxy-2-hydroxybenzaldehydes, followed by reductive amination with sodium borohydride. While the first step of this reaction is predictable, the subsequent reductive amination can result in either mono-, di- or tri(alkoxy-hydroxybenzyl)-DAZA compounds. Seeking to identify dependencies that might allow a specific reaction control towards the formation of either of the three possible products, and particularly towards the favoured trialkylated DAZA compounds, a variety of synthesis trials were performed. Additionally, computational methods were employed to evaluate the underlying reaction mechanism. Synthesis trials verified that the trialkylated DAZA compounds are formed via direct reductive amination of the dialkylated DAZA compounds. Subsequently, a synthetic method was established, leading to an increase in the percentage of the trialkylated DAZA compounds, which allowed the successful isolation of those hexadentate chelators. Additionally, an alternative pathway proceeding via aminal C–N bond insertion of an attacking third carbonyl moiety was evaluated by means of quantum chemical calculations but so far remains entirely hypothetical.

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