157920-22-4Relevant academic research and scientific papers
Fructose 1,6-bisphosphate aldolase from Staphylococcus carnosus: Overexpression, structure prediction, stereoselectivity, and application in the synthesis of bicyclic sugars
Zannetti, Maria Teresa,Walter, Christiane,Knorst, Marion,Fessner, Wolf-Dieter
, p. 1882 - 1890 (1999)
The gene for the fructose 1,6-bisphosphate aldolase from Staphylococcus carnosus (FruA(sca)) was subcloned for overexpression in Escherichia coli using the expression vector pKK223-3. An efficient, single-step purification by DEAE ion-exchange chromatography furnished the recombinant enzyme ready for synthetic applications. Sequence analysis indicated that FruA(sca) shares the overall α/β-barrel structure and most of the active site residues with the structurally well-defined FruA catalyst from rabbit muscle which signaled its functional equivalence for synthetic applications. A preparative study with generic aliphatic and hydroxylated aldehydes indeed confirmed a high level of stereoselectivity for both newly created asymmetric centers, and suggested a kinetic enantioselectivity for anionically charged 3- hydroxyaldehydes. In fact, the monomeric FruA(sca) was found to tolerate even the presence of highly reactive glutardialdehyde derivatives, which otherwise rapidly denature the rabbit muscle enzyme, and to allow their stereoselective conversion to bicyclic sugars.
From the North Sea to Drug Repurposing, the Antiseizure Activity of Halimide and Plinabulin
Copmans, Dani?lle,Crawford, Alexander D.,De Borggraeve, Wim M.,Esguerra, Camila V.,Kildgaard, Sara,Larsen, Thomas O.,Partoens, Michèle,Roux, Emma,Steurs, Gert,Wang, Xinhui,de Witte, Peter A. M.
, (2022/03/01)
PharmaSea performed large-scale in vivo screening of marine natural product (MNP) ex-tracts, using zebrafish embryos and larvae, to identify compounds with the potential to treat epilepsy. In this study, we report the discovery of two new antiseizure comp
HETEROARYLDIHYDROPYRIMIDINE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
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Page/Page column 62; 63, (2019/01/17)
Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
SPIRO-OXAZOLONES
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Page/Page column 79, (2015/09/28)
The present invention provides spiro-oxazolones, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The present compounds are useful as therapeutics acting peripherally and centrally in the conditions of inappropriate secretion of vasopressin, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, aggressive behavior and phase shift sleep disorders, in particular jetlag.
Lewis acid catalyzed synthesis of cyclic carbonates, precursors of 1,2- and 1,3-diols
Cornil, Johan,Gonnard, Laurine,Guerinot, Amandine,Reymond, Sebastien,Cossy, Janine
supporting information, p. 4958 - 4962 (2014/08/18)
An eco-friendly synthesis of cyclic carbonates through a Lewis acid catalyzed cyclization of tert-butyl carbonates is described. These cyclic carbonates are precursors of 1,2- and 1,3-diols, and the developed method was applied to a short synthesis of a diarylheptanoid, (3S,5S)-alpinikatin.
FeCl3·6H2O, a catalyst for the diastereoselective synthesis of cis-isoxazolidines from N-protected δ-hydroxylamino allylic acetates
Cornil, Johan,Guerinot, Amandine,Reymond, Sebastien,Cossy, Janine
, p. 10273 - 10287 (2013/11/06)
An ecofriendly and diastereoselective synthesis of cis-3,5-disubstituted isoxazolidines through the FeCl3·6H2O-catalyzed cyclization of δ-hydroxylamino allylic acetates is described. The synthetic potential of these products is highlighted by the preparation of several functionalized 1,3-amino alcohol precursors.
Radical cyclization of α-bromo aluminum acetals onto alkenes and alkynes (radic[al] process): A simple access to γ-lactols and 4-methylene-γ-lactols
Boussonniere, Anne,Beneteau, Romain,Zimmermann, Nicolas,Lebreton, Jacques,Denes, Fabrice
supporting information; experimental part, p. 5613 - 5627 (2011/06/22)
An efficient preparation of γ-lactols and methylene-γ-lactols is described. Highly acid-sensitive lactols are prepared in a concise manner by using a radical cyclization of aluminum acetals. The precursors for the radical reactions are readily prepared fr
Dynamic kinetic resolution of α-substituted β-ketoesters catalyzed by Baeyer-Villiger monooxygenases: Access to enantiopure α-hydroxy esters
Rioz-Martínez, Ana,Cuetos, Aníbal,Rodríguez, Cristina,De Gonzalo, Gonzalo,Lavandera, Iván,Fraaije, Marco W.,Gotor, Vicente
supporting information; experimental part, p. 8387 - 8390 (2011/10/09)
BVMOs make a play: The dynamic kinetic resolution of racemic α-alkyl-β-ketoesters was performed through a selective Baeyer-Villiger oxidation employing different Baeyer-Villiger monooxygenases (BVMOs) in mild basic media. The product diesters were obtained with excellent yields and enantioselectivities, and used as precursors for optically active α-hydroxy esters.
Construction of carbo- And heterocycles using radical relay cyclizations initiated by alkoxy radicals
Zhu, Hai,Wickenden, Jason G.,Campbell, Natalie E.,Leung, Joe C. T.,Johnson, Kayli M.,Sammis, Glenn M.
supporting information; experimental part, p. 2019 - 2022 (2009/09/08)
An efficient method for the rapid construction of carbo- and heterocycles has been developed using radical relay cyclizations initiated by alkoxy radicals. Linear substrates were cyclized to form a wide range of cyclopentane, pyrrolidine, tetrahydropyran, and tetrahydrofuran derivatives in excellent yields. This methodology was utilized as a key step in the synthesis of the tetrahydrofuran fragment in (-)-amphidino-lide K.
Bis(NHC)-Pd(II) complexes as highly efficient catalysts for allylation of aldehydes with allyltributyltin
Zhang, Tao,Shi, Min,Zhao, Meixin
, p. 2412 - 2418 (2008/09/18)
Novel cis-chelated bidentate bis(NHC)-Pd(II) complexes derived from 1,1′-binaphthyl-2,2′-diamine (BINAM) bearing weakly coordinating acetate or trifluoroacetate counterions have been synthesized and their structures have been characterized by X-ray diffra
