50817-56-6Relevant academic research and scientific papers
Silver triflate catalyzed tandem heterocyclization/alkynylation of 1-((2-tosylamino)aryl)but-2-yne-1,4-diols to 2-alkynyl indoles
Mothe, Srinivasa Reddy,Kothandaraman, Prasath,Lauw, Sherman Jun Liang,Chin, Samuel Ming Wei,Chan, Philip Wai Hong
supporting information; experimental part, p. 6133 - 6137 (2012/06/30)
Don't cross me! 2-Alkynyl indoles were prepared efficiently by the AgOTf-catalyzed tandem heterocyclization/alkynylation of 1-(2-tosylamino)aryl) but-2-yne-1,4-diols under mild conditions (see scheme). The attractiveness of this approach lies in the fact that both the indole ring and alkyne side chain of the N-heterocycle are sequentially formed from low cost, readily available, and ecologically benign starting materials. It also provides the first route to this synthetically valuable class of compounds that is not based on a cross-coupling strategy. Copyright
COX-1/COX-2 inhibitors based on the methanone moiety
Dannhardt, Gerd,Fiebich, Bernd L,Schweppenhaeuser, Johannes
, p. 147 - 161 (2007/10/03)
This paper focuses on the synthesis and the in vitro testing of dual COX-1/COX-2 inhibitors. Starting from structures of non-steroidal anti-inflammatory drugs (NSAIDs) the diaryl methanone element was chosen as a lead. Modifications were carried out on this scaffold to obtain potent inhibitors of the COX enzymes. The N-(2-aroylphenyl)sulphonamides and -amides were studied in detail, and to consolidate the data evaluated the corresponding 3- and 4-regioisomers were also investigated. The potency and the enzyme selectivity were varied by structural modifications of the lead.
