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Synthesis of C-11-labeled Sulfonyl Carbamates through a Multicomponent Reaction Employing Sulfonyl Azides, Alcohols, and [C-11]CO
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry.ORCID iD: 0000-0002-9441-3767
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Division of Molecular Imaging.ORCID iD: E-8373-2012
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2016 (English)In: ChemistryOpen, ISSN 2191-1363, Vol. 5, no 6, p. 566-573Article in journal (Refereed) Published
Abstract [en]

We describe the development of a new methodology focusing on C-11-labeling of sulfonyl carbamates in a multicomponent reaction comprised of a sulfonyl azide, an alkyl alcohol, and [C-11] CO. A number of C-11-labeled sulfonyl carbamates were synthesized and isolated, and the developed methodology was then applied in the preparation of a biologically active molecule. The target compound was obtained in 24 +/- 10% isolated radiochemical yield and was evaluated for binding properties in a tumor cell assay; in vivo biodistribution and imaging studies were also performed. This represents the first successful radiolabeling of a non-peptide angiotensin II receptor subtype 2 agonist, C21, currently in clinical trials for the treatment of idiopathic pulmonary fibrosis.

Place, publisher, year, edition, pages
2016. Vol. 5, no 6, p. 566-573
Keywords [en]
AT(2)R agonists, multicomponent reactions, radiochemistry, sulfonyl azides, sulfonyl carbamates
National Category
Medicinal Chemistry
Identifiers
URN: urn:nbn:se:uu:diva-316971DOI: 10.1002/open.201600091ISI: 000393071500012PubMedID: 28032026OAI: oai:DiVA.org:uu-316971DiVA, id: diva2:1079445
Funder
Carl Tryggers foundation , CTS13:333 CTS14:356Swedish Cancer Society, 2014/474Swedish Research Council, 2015-02509Available from: 2017-03-08 Created: 2017-03-08 Last updated: 2018-01-13Bibliographically approved

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Stevens, Marc Y.Chow, Shiao Y.Estrada, SergioEriksson, JonasAsplund, VeronikaOrlova, AnnaMitran, BogdanAntoni, GunnarLarhed, MatsÅberg, OlaOdell, Luke R.
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Organic Pharmaceutical ChemistryDepartment of Medicinal ChemistryDivision of Molecular ImagingScience for Life Laboratory, SciLifeLab
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