29146-63-2Relevant academic research and scientific papers
Novel non-peptidic small molecule inhibitors of secreted aspartic protease 2 (SAP2) for the treatment of resistant fungal infections
Dong, Guoqiang,Liu, Yang,Wu, Ying,Tu, Jie,Chen, Shuqiang,Liu, Na,Sheng, Chunquan
supporting information, p. 13535 - 13538 (2019/01/05)
Targeting secreted aspartic protease 2 (SAP2), a kind of virulence factor, represents a new strategy for antifungal drug discovery. In this report, the first-generation of small molecule SAP2 inhibitors was rationally designed and optimized using a structure-based approach. In particular, inhibitor 23h was highly potent and selective and showed good antifungal potency for the treatment of resistant Candida albicans infections.
A Bench-Stable Vilsmeier Reagent for in situ Alcohol Activation: Synthetic Application in the Synthesis of 2-Amino-2-Thiazolines
Corbett, Michael T.,Caille, Seb
supporting information, p. 2845 - 2850 (2017/10/06)
A robust, chemoselective direct condensation/cyclization of thioureas and amino alcohols is described. Employing a bench-stable Vilsmeier reagent, methoxymethylene- N, N -dimethyliminium methyl sulfate, the selective in situ activation of alcohols is achieved with high efficiency and broad functional-group tolerance. The reversible interaction of the Vilsmeier reagent with substrate was key to the success of this activation strategy.
Synthesis of benzimidazole-fused heterocycles by intramolecular oxidative C-N bond formation using hypervalent iodine reagents
Kutsumura, Noriki,Kunimatsu, Shinichi,Kagawa, Kimiko,Otani, Takashi,Saito, Takao
experimental part, p. 3235 - 3240 (2011/11/30)
A straightforward approach by dehydrogenative C-N coupling between aryl C-H and N-H bonds using a hypervalent iodine reagent under mild conditions offers a versatile and convenient method for synthesizing various benzimidazole-fused heterocycles. Georg Th
A convenient method for the synthesis of 2-amino substituted aza-heterocycles from N,N′-disubstituted thioureas using TsCl/NaOH
Heinelt, Uwe,Schultheis, Daniela,J?ger, Siegfried,Lindenmaier, Marion,Pollex, Annett,Beckmann, Henning S.G.
, p. 9883 - 9888 (2007/10/03)
p-Toluenesulfonyl chloride (TsCl)/NaOH has been introduced as reagent combination for the synthesis of 2-amino-oxa- or 2-amino-thiazolidines from N-(2-hydroxyethyl)-thioureas, but its general application in heterocycle synthesis has not been investigated. In this paper the convenient and efficient synthesis of a variety of 2-amino-substituted 1-aza 3-(aza, oxo or thio) heterocycles of different substitution and ring sizes is described. The application of polymer-supported TsCl facilitates work-up and renders the reaction conditions very suitable for parallel or robot synthesis. Graphical Abstract
Process for synthesizing heterocyclic compounds
-
Page/Page column 9, (2008/06/13)
The invention provides the process illustrated in scheme 1 for synthesizing heterocyclic compounds of formula I. In the process, an isothiocyanate of formula II is initially reacted with a primary amine of formula III to give a thiourea of formula IV. Subsequently, the thiourea of formula IV is converted to the corresponding heterocycle of formula I using a base and a sulfonyl chloride.
Aminothiazines et aminothiazoles analogues ouverts du levamisole: synthese et approche du mode d'action nematicide
Caujolle, Raymond,Amarouch, Hamid,Payard, Marc,Loiseau, Philippe R.,Bories, Christian,et al.
, p. 287 - 292 (2007/10/02)
New compounds with thiazoline or dihydrothiazine rings substituted by alkylamino or arylamino groups were synthesized and screened in vitro against three Nematodes.Inhibition of fumarate-reductase activity was also evaluated.For all in vitro anti-parasitic tests, dihydrothiazines were more potent than corresponding thiazolines derivatives, however, thiazolines showed a greater inhibition of fumarate-reductase.
