141764-83-2Relevant academic research and scientific papers
Discovery and hit-to-lead optimization of novel allosteric glucokinase activators
Lang, Martin,Seifert, Markus H.-J.,Wolf, Kristina K.,Aschenbrenner, Andrea,Baumgartner, Roland,Wieber, Tanja,Trentinaglia, Viola,Blisse, Marcus,Tajima, Nobumitsu,Yamashita, Tokuyuki,Vitt, Daniel,Noda, Hitoshi
supporting information; scheme or table, p. 5417 - 5422 (2011/10/12)
We report on a hit generation and hit-to-lead program of a novel class of glucokinase activators (GKAs). Hit compounds, activators at low glucose concentration only were identified by vHTS. Scaffold modification reliably afforded activators also at high s
New methodology for 2-alkylation of 3-furoic acids: Application to the synthesis of tethered UC-781/d4T bifunctional HIV reverse-transcriptase inhibitors
Arnott, Gareth,Hunter, Roger,Mbeki, Linda,Mohamed, Ebrahim
, p. 4023 - 4026 (2007/10/03)
New methodology for 2-alkylation of 3-furoic acids is presented involving Wittig reactions of the 3-methoxycarbonyl-2-furanylmethylphosphonium salt. The methodology has been used to prepare a tethered 2-alkylated-UC-781/d4T conjugate as a potentially new type of HIV reverse-transcriptase inhibitor.
An Improved Synthesis of 2-Substituted-3-furoic Acids Leading to an Intramolecular Diels-Alder Reaction Between a Dienophile and Furan Diene Both Containing an Electron Withdrawing Group
Yu, Shuyuan,Beese, Giovanna,Keay, Brian A.
, p. 2729 - 2734 (2007/10/02)
An improved preparation of various 2-substituted-3-furoic acids by lithiation of 2-methyl-3-furoic acid with 2.0 equiv. of butyllithium, and a successful intramolecular Diels-Alder reaction using 0.1 equiv. of methylaluminium dichloride between a dienophi
Unsaturated Sulfoxides in Organic Synthesis: A New General Furan Synthesis
Chan, Wing Hong,Lee, Albert W. M.,Chan, Eddy T. T.
, p. 945 - 946 (2007/10/02)
Furans have been efficiently synthesised by a three-step reaction sequence.Michael addition of keto esters to alkenyl sulfoxides followed by Pummerer rearrangement afforded the cyclic intermediates 11 in good yield.Treatment of the latter with 3-chloroperoxybenzoic acid led by oxidation and syn-elimination of the corresponding sulfoxide, to substituted furans.
