449780-22-7Relevant academic research and scientific papers
Development of new thiazole-based iridium catalysts and their applications in the asymmetric hydrogenation of trisubstituted olefins
Cheruku, Pradeep,Paptchikhine, Alexander,Ali, Muhammad,Neudoerfl, Joerg-M.,Andersson, Pher G.
, p. 366 - 373 (2008/10/09)
New thiazole-based chiral N,P-ligands that are open-chain analogues of known cyclic thiazole ligands have been synthesized and evaluated in the iridium-catalyzed asymmetric hydrogenation of trisubstituted olefins. Chirality was introduced into the ligands through a highly diastereoselective alkylation using Oppolzer's camphorsultam as chiral auxiliary. In general, the new catalysts are as reactive and selective as their cyclic counterparts for the asymmetric hydrogenation of various trisubstituted olefins. This journal is The Royal Society of Chemistry.
Synthesis and antifungal activity evaluation of 3-hetaryl-2,5-dihydrofuran-2-ones. An unusual fragmentation of the oxazole ring via 2,3-selenoxide shift
Kunes, Jiri,Balsanek, Vojtech,Pour, Milan,Buchta, Vladimir
, p. 1809 - 1830 (2007/10/03)
In continuing the studies on the synthesis and evaluation of antifungal activity of the analogues of (-)incrustoporine, the replacement of the phenyl moiety at C3 of the furanone ring with a hetaryl substituent was considered. Thus, a series of 5-alkyl-3-hetaryl-2,5-dihydrofuran-2-ones with the thienyl, furyl and thiazolyl moieties attached to C3 was synthesized, and the compounds subjected to antifungal activity screening. In the preparation of compounds containing the oxazolyl fragment, the [2,3]-sigmatropic rearrangement led to the fragmentation of the oxazole ring, resulting in the formation of 3-(1-benzamido-2-oxoethylidene)-5-methyltetrahydrofuran-2-one. Somewhat surprisingly, the antifungal efficiency of the derivatives was lower in comparison with analogues containing a substituted phenyl at C3.
Azole phenoxy hydroxyureas as selective and orally active inhibitors of 5- lipoxygenase
Malamas,Carlson,Grimes,Howell,Glaser,Gunawan,Nelson,Kanzelberger,Shah,Hartman
, p. 237 - 245 (2007/10/03)
Azole phenoxy hydroxyureas are a new class of 5-lipoxygenase (5-LO) inhibitors. Structure-activity relationship studies have demonstrated that electronegative substituents on the 2-phenyl portion of the oxazole tail increased the ex vivo potency of these
