Now showing items 1-10 of 17
A Concise Total Synthesis of Breitfussin A and B
(Journal article; Tidsskriftartikkel; Peer reviewed, 2014)
Enantioselective incorporation of CO2: status and potential
(Journal article; Tidsskriftartikkel; Peer reviewed, 2017-09-09)
CO<sub>2</sub> is a promising and sustainable carbon feedstock for organic synthesis. New catalytic protocols for efficient incorporation of CO<sub>2</sub>into organic molecules are continuously being reported. However, little progress has been made in the enantioselective conversion of CO<sub>2</sub>to form enantioenriched molecules. In order to allow CO<sub>2</sub>to become a versatile carbon ...
Experimental and four-component relativistic DFT studies of tungsten carbonyl complexes
(Journal article; Tidsskriftartikkel; Peer reviewed, 2015-07-24)
We present a theoretical and experimental study of the structure and nuclear magnetic resonance (NMR) parameters of the pentacarbonyltungsten complexes of η<sup>1</sup>-2-(trimethylstannyl)-4,5-dimethylphosphinine, η<sup>2</sup>-norbornene, and imidazolidine-2-thione. The three complexes have a pseudo-octahedral molecular structure with the six ligands bonded to the tungsten atom. The η<sup>1</sup ...
Iridium-PHOX-mediated alkene hydrogenation: Isomerisation influences the stereochemical outcome
(Journal article; Tidsskriftartikkel; Peer reviewed, 2014-05-27)
Recent experimental studies of iridium-phosphinooxazoline-mediated alkene hydrogenation indicated two dihydride species as resting states, with the minor isomer assumed to give rise to the major product enantiomer [Gruber and Pfaltz, Angew. Chem. Int. Ed. 2014, 53, 1896]. B3LYP-D2 calculations confirm the two dihydride intermediates as resting states but show that these species do not give rise to ...
Palladium(0)-Catalyzed Cross-Couplings of 2-Bromophosphinine
(Journal article; Tidsskriftartikkel; Peer reviewed, 2013-05-21)
A new Negishi-type cross-coupling of 2-bromophosphinine has been developed. The new method expands the scope of palladium-catalyzed couplings to monobromophosphinines, which have been considered as poor substrates so far. Moreover, aryl-, alkenyl-, and alkynylzinc bromides were found to be effective coupling partners.
Total synthesis of tubastrine and 3-dehydroxy tubastrine by microwave-assisted cross-coupling reactions
(Journal article; Tidsskriftartikkel; Peer reviewed, 2015-09-03)
The first syntheses of tubastrine and 3-dehydroxy tubastrine are described. The target compounds were prepared in four consecutive steps from commercially available starting materials. The central scaffold was formed by a microwave-assisted C–N cross-coupling reaction between 1,3-bis(<i>tert</i>-butoxycarbonyl)-guanidine and (<i>E</i>)-((4-(2-iodovinyl)-1,2-phenylene)bis(oxy))bis(<i>tert</i>-butyl ...
Metallo-β-lactamase inhibitors by bioisosteric replacement: preparation, activity and binding
(Journal article; Tidsskriftartikkel; Peer reviewed, 2017-04-14)
Bacterial resistance is compromising the use of β-lactam antibiotics including carbapenems. The main resistance mechanism against β-lactams is hydrolysis of the β-lactam ring mediated by serine- or metallo-β-lactamases (MBLs). Although several inhibitors of MBLs have been reported, none has been developed into a clinically useful inhibitor. Mercaptocarboxylic acids are among the most prominent ...
Aldol condensations on a 3-alkylidene-2,5-diketopiperazine - synthesis of two marine natural products
(Journal article; Tidsskriftartikkel; Peer reviewed, 2018-06)
The synthesis of two marine natural products containing a 3-alkylidene-6-arylidene-2,5-diketopiperazine scaffold by employing two consecutive aldol condensations starting with 1,4-diacetyl-2,5-diketopiperazine is reported. The target compounds contain a phenol or an imidazole group as aryl substituents, respectively, and suitable conditions for the aldol condensation of 1-acyl-3-alkylidene-2,5-dik ...
Rhodium-Catalyzed Synthesis of Sulfur Ylides via in Situ Generated Iodonium Ylides
(Journal article; Tidsskriftartikkel; Peer reviewed, 2017-11-22)
A convenient strategy for the synthesis of sulfur ylides via rhodium-catalyzed coupling of in situ generated iodonium ylides with sulfides or sulfoxides has been developed. A wide range of sulfur ylides were obtained in moderate to good yields from inexpensive sulfur compounds and active methylene compounds with a short reaction time (MW, 5–10 min) or 12–16 h at rt. Furthermore, these sulfoxonium ...
A focused fragment library targeting the antibiotic resistance enzyme - Oxacillinase-48: Synthesis, structural evaluation and inhibitor design
(Journal article; Tidsskriftartikkel; Peer reviewed, 2018-02-10)
β-Lactam antibiotics are of utmost importance when treating bacterial infections in the medical community. However, currently their utility is threatened by the emergence and spread of β-lactam resistance. The most prevalent resistance mechanism to β-lactam antibiotics is expression of β-lactamase enzymes. One way to overcome resistance caused by β-lactamases, is the development of β-lactamase ...