“…2 Thiophenes are an important class of heterocyclic compounds with applications in the design of advanced materials to the treatment of various diseases. In particular, 2,3-diarylthiophenes have been shown to selectively inhibit the cycloxygenase-2 (COX-2) enzyme, [10][11][12][13] which is induced during inflammatory conditions. DuP 697 (1) is one of the earliest members of this tricyclic class of inhibitors and it is moderately selective for COX-2.…”
Section: Introductionmentioning
confidence: 99%
“…Thus, DuP 697 provides an intriguing backdrop for honing synthetic strategies for drug development. The first published synthesis of DuP 697 (Scheme 1) 11 was linear and involved construction of the thiophene ring from appropriate starting materials. It is interesting that a literature search of 2bromothiophenes that bear cyclic substituents at the 4 and 5-positions yields only 56 compounds, 28 of which have been the subject of biological studies.…”
C-H activation/borylation has been married with Suzuki coupling to prepare DuP 697 (1) and analogs that would be otherwise difficult to obtain via the traditional synthetic route to 1.
“…2 Thiophenes are an important class of heterocyclic compounds with applications in the design of advanced materials to the treatment of various diseases. In particular, 2,3-diarylthiophenes have been shown to selectively inhibit the cycloxygenase-2 (COX-2) enzyme, [10][11][12][13] which is induced during inflammatory conditions. DuP 697 (1) is one of the earliest members of this tricyclic class of inhibitors and it is moderately selective for COX-2.…”
Section: Introductionmentioning
confidence: 99%
“…Thus, DuP 697 provides an intriguing backdrop for honing synthetic strategies for drug development. The first published synthesis of DuP 697 (Scheme 1) 11 was linear and involved construction of the thiophene ring from appropriate starting materials. It is interesting that a literature search of 2bromothiophenes that bear cyclic substituents at the 4 and 5-positions yields only 56 compounds, 28 of which have been the subject of biological studies.…”
C-H activation/borylation has been married with Suzuki coupling to prepare DuP 697 (1) and analogs that would be otherwise difficult to obtain via the traditional synthetic route to 1.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.