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- Title
Synthesis of <sup>11</sup>C‐labeled Sulfonyl Carbamates through a Multicomponent Reaction Employing Sulfonyl Azides, Alcohols, and [<sup>11</sup>C]CO.
- Authors
Stevens, Marc Y.; Chow, Shiao Y.; Odell, Luke R.; Estrada, Sergio; Asplund, Veronika; Åberg, Ola; Eriksson, Jonas; Orlova, Anna; Mitran, Bogdan; Antoni, Gunnar; Larhed, Mats
- Abstract
Abstract: We describe the development of a new methodology focusing on 11C‐labeling of sulfonyl carbamates in a multicomponent reaction comprised of a sulfonyl azide, an alkyl alcohol, and [11C]CO. A number of 11C‐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.
- Subjects
CARBAMATES synthesis; SULFONYL azides; ALCOHOLS (Chemical class); RADIOCHEMICAL analysis; MULTIPHASE flow
- Publication
ChemistryOpen, 2016, Vol 5, Issue 6, p566
- ISSN
2191-1363
- Publication type
Article
- DOI
10.1002/open.201600091