@article{f011be2b3c104e06a96d1b72bf54c5c2,
title = "Synthesis of 11C-labeled Sulfonyl Carbamates through a Multicomponent Reaction Employing Sulfonyl Azides, Alcohols, and [11C]CO",
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.",
keywords = "ATR agonists, multicomponent reactions, radiochemistry, sulfonyl azides, sulfonyl carbamates",
author = "Stevens, {Marc Y.} and Chow, {Shiao Y.} and Sergio Estrada and Jonas Eriksson and Veronika Asplund and Anna Orlova and Bogdan Mitran and Gunnar Antoni and Mats Larhed and Ola {\AA}berg and Odell, {Luke R.}",
note = "Funding Information: This work was supported by the Carl Tryggers Foundation for Scientific Research (CTS13:333, CTS14:356), Cancerfonden (Swedish Cancer Society, 2014/474), Vetenskapsr?det Swedish Research Council (2015-02509), and Uppsala University. The authors wish to thank Helena Wilking and Margareta Sprycha (Uppsala University Hospital) for assistance with radio-MS and Dr. Lisa Haigh (Imperial College London) for performing accurate mass studies. Dr. Patrik Nordeman (Uppsala University Hospital) and Dr. Charlotta Wallinder (Uppsala Univeristy) are acknowledged for fruitful discussions. Publisher Copyright: {\textcopyright} 2016 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA. Copyright: Copyright 2016 Elsevier B.V., All rights reserved.",
year = "2016",
month = dec,
day = "1",
doi = "10.1002/open.201600091",
language = "English",
volume = "5",
pages = "566--573",
journal = "ChemistryOpen",
issn = "2191-1363",
publisher = "John Wiley and Sons Inc.",
number = "6",
}