<sup>211</sup>At and <sup>125</sup>I‐Labeling of (Hetero)Aryliodonium Ylides: Astatine Wins Again

Maingueneau, Clémence; Berdal, Marion; Eychenne, Romain; Gaschet, Joëlle; Chérel, Michel; Gestin, Jean‐François; Guérard, François

doi:10.1002/chem.202104169

Cited by 11 publications

(4 citation statements)

References 30 publications

(57 reference statements)

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“…Evaporating Chloroform Eluate creating a dry residue of astatine is often used as a starting point for many different types of chemical reactions and applications, both organic and aqueous 18 – 20 . Trying to elucidate the actual astatine speciation in the dry form of Chloroform Eluate is naturally difficult.…”

Section: Resultsmentioning

confidence: 99%

Behaviour, use and safety aspects of astatine-211 solvated in chloroform after dry distillation recovery

Aneheim,

Hansson,

Timperanza

et al. 2024

Sci Rep

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Targeted alpha therapy of disseminated cancer is an emerging technique where astatine-211 is one of the most promising candidate nuclides. Astatine-211 can be produced in medium energy cyclotrons by alpha particle bombardment of natural bismuth. The produced astatine is then commonly recovered from the irradiated solid target material through dry distillation. The dry distillation process often includes elution and solvation of condensed astatine with chloroform, forming Chloroform Eluate. In this work the handling and safe use of the high activity concentration Chloroform Eluate has been investigated. Correctly performed, evaporation of Chloroform Eluate results in a dry residue with complete recovery of the astatine. The dry residue can then serve as a versatile starting material, using appropriate oxidizing or reducing conditions, for subsequent downstream chemistry. However, it has been found that when evaporating the Chloroform Eluate, astatine can be volatilized if continuing the process beyond the point of dryness. This behavior is more pronounced when the Chloroform Eluate has received a higher absorbed dose. Upon water phase contact of the Chloroform Eluate, a major part of the astatine activity becomes water soluble, leaving the organic phase. A behavior which is also dependent on dose to the solvent.

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Section: Resultsmentioning

confidence: 99%

Behaviour, use and safety aspects of astatine-211 solvated in chloroform after dry distillation recovery

Aneheim,

Hansson,

Timperanza

et al. 2024

Sci Rep

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“…Therefore, we believe that potassium carbonate simply increases the nucleophilicity of the astatine species when isolated by dry distillation. 11 Astatine from dry distillation, however, is known to contain a variety of oxidated astatines 12 and requires a reducing agent prior to use in nucleophilic substitution. 13 Based on the reaction mechanism of DMSO oxidation of alkyl halides to aldehydes, it seemed logical that a precursor of highly reactive neopentyl sulfonyl ester might reduce the oxidated astatine species to astatine under basic conditions.…”

Section: Resultsmentioning

confidence: 99%

1-(N,N-Dialkylcarbamoyl)-1,1-difluoromethanesulfonyl ester as a stable and effective precursor for a neopentyl labeling group with astatine-211

Sasaki,

Tada,

Liu

et al. 2023

Org. Biomol. Chem.

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“…Other methods such as using aryliodonium ylides for the introduction of nucleophilic astatine have been reported to generate a wide new range of PGs [ 93 ]. Despite their wide use, PGs containing activated esters have several limitations.…”

Section: Bioconjugation Strategiesmentioning

confidence: 99%

Optimizing the Safety and Efficacy of Bio-Radiopharmaceuticals for Cancer Therapy

et al. 2023

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The precise delivery of cytotoxic radiation to cancer cells through the combination of a specific targeting vector with a radionuclide for targeted radionuclide therapy (TRT) has proven valuable for cancer care. TRT is increasingly being considered a relevant treatment method in fighting micro-metastases in the case of relapsed and disseminated disease. While antibodies were the first vectors applied in TRT, increasing research data has cited antibody fragments and peptides with superior properties and thus a growing interest in application. As further studies are completed and the need for novel radiopharmaceuticals nurtures, rigorous considerations in the design, laboratory analysis, pre-clinical evaluation, and clinical translation must be considered to ensure improved safety and effectiveness. Here, we assess the status and recent development of biological-based radiopharmaceuticals, with a focus on peptides and antibody fragments. Challenges in radiopharmaceutical design range from target selection, vector design, choice of radionuclides and associated radiochemistry. Dosimetry estimation, and the assessment of mechanisms to increase tumor uptake while reducing off-target exposure are discussed.

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²¹¹At and ¹²⁵I‐Labeling of (Hetero)Aryliodonium Ylides: Astatine Wins Again

Abstract: Supporting information for this article is given via a link at the end of the document.

Cited by 11 publications

References 30 publications

Behaviour, use and safety aspects of astatine-211 solvated in chloroform after dry distillation recovery

Behaviour, use and safety aspects of astatine-211 solvated in chloroform after dry distillation recovery

1-(N,N-Dialkylcarbamoyl)-1,1-difluoromethanesulfonyl ester as a stable and effective precursor for a neopentyl labeling group with astatine-211

Optimizing the Safety and Efficacy of Bio-Radiopharmaceuticals for Cancer Therapy

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211At and 125I‐Labeling of (Hetero)Aryliodonium Ylides: Astatine Wins Again

Abstract: Supporting information for this article is given via a link at the end of the document.

Cited by 11 publications

References 30 publications

Behaviour, use and safety aspects of astatine-211 solvated in chloroform after dry distillation recovery

Behaviour, use and safety aspects of astatine-211 solvated in chloroform after dry distillation recovery

1-(N,N-Dialkylcarbamoyl)-1,1-difluoromethanesulfonyl ester as a stable and effective precursor for a neopentyl labeling group with astatine-211

Optimizing the Safety and Efficacy of Bio-Radiopharmaceuticals for Cancer Therapy

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²¹¹At and ¹²⁵I‐Labeling of (Hetero)Aryliodonium Ylides: Astatine Wins Again