Please use this identifier to cite or link to this item: https://hdl.handle.net/1959.11/7539
Title: Tandem free-radical addition/substitution chemistry and its application to the preparation of novel AT₁ receptor antagonists
Contributor(s): Staples, Maree K (author); Grange, Rebecca L (author); Angus, James A (author); Ziogas, James (author); Tan, Nichole P H (author); Taylor, Michelle Keily (author); Schiesser, Carl H (author)
Publication Date: 2011
DOI: 10.1039/c0ob00573h
Handle Link: https://hdl.handle.net/1959.11/7539
Abstract: Benzothiophene and benzoselenophene analogues of the thiophene-containing antihypertensives milfasartan and eprosartan were prepared and tested for AT1 receptor antagonist properties. While the sulfur-containing systems were prepared following existing methodology, the selenium-containing analogues required the development of novel, tandem free-radical chemistry involving addition of aryl radicals to alkynes, followed by intramolecular homolytic substitution at the higher heteroatom. All four compounds prepared proved to be excellent AT₁ receptor antagonists, with pKв estimates of 7.2-9.5.
Publication Type: Journal Article
Source of Publication: Organic & Biomolecular Chemistry, 9(2), p. 473-479
Publisher: Royal Society of Chemistry
Place of Publication: United Kingdom
ISSN: 1477-0520
1477-0539
Field of Research (FOR): 030501 Free Radical Chemistry
030503 Organic Chemical Synthesis
030401 Biologically Active Molecules
Peer Reviewed: Yes
HERDC Category Description: C1 Refereed Article in a Scholarly Journal
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