Journal of Combinatorial Chemistry
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S(N)Ar-based, facile synthesis of a library of benzothiaoxazepine-1,1'-dioxides.
The construction of a library of benzothiaoxazepine-1,1'-dioxides utilizing a one-pot, S(N)Ar diversification-ODCT(50) scavenging protocol is reported. This protocol combines microwave irradiation to facilitate the reaction, in conjunction with a soluble ROMP-derived scavenger (ODCT) to afford the d...
Fluorous tagged N-hydroxy phthalimide for the parallel synthesis of O-aryloxyamines.
The parallel synthesis of O-aryloxyamines remains an unfulfilled need in the field of medicinal chemistry and fragment-based approaches. To fill this gap a solution-phase two-step process based on (1) a copper-catalyzed cross-coupling of aryl boronic acids with a fluorous tagged N-hydroxyphthalimide...
Novel isocyanide-based one-pot multicomponent syntheses of tetrahydrobenzo[b][1,4]oxazepine and malonamide derivatives.
In this work, a novel one-pot multicomponent reaction of 2-aminophenols, Meldrum's acid, and isocyanides leads to the synthesis of tetrahydrobenzo[b][1,4]oxazepine or malonamide derivatives using 1 or 2 equiv of 2-aminophenols, respectively, in good to excellent yields at ambient temperature.
Concise synthesis of 2, 3-diarylpyrimido[1,2-a]benzimidazole based on isoflavones.
The 2,3-diarylpyrimido[1,2-a]benzimidazole derivatives were prepared by one-step cyclocondensation of 2-aminobenzimidazole with isoflavone in methanol. Single-crystal diffraction analysis was performed for 2-(2-hydroxyl-4-isopropoxy-phenyl)-3-phenylpyrimido[1,2-a]benzimidazole. The fluorescence prop...
Solution-phase parallel synthesis of novel membrane-targeted antibiotics.
We described a series of benzophenone-containing antibiotics which displayed activity against antibiotic-resistant bacteria. We have shown that these agents function by disrupting the bacterial membrane. To further explore these compounds, a practical and efficient solution-phase parallel synthesis...
Combinatorial materials research applied to the development of new surface coatings XIII: an investigation of polysiloxane antimicrobial coa...
High-throughput biological assays were used to develop structure - antimicrobial relationships for polysiloxane coatings containing chemically bound (tethered) quaternary ammonium salt (QAS) moieties. The QAS-functional polysiloxanes were derived from solution blends of a silanol-ter...
2-Substituted-4,5-dihydroxypyrimidine-6-carboxamide antiviral targeted libraries.
We have developed the parallel synthesis of a structurally interesting class of 2-substituted-4,5-dihydroxypyrimidine-6-carboxamides. Variously 2-substituted-4,5-dihydroxypyrimidine-6-carboxylate methyl esters were initially prepared and were then diversified via a facile amidation reaction. This st...
Combinatorial/high throughput methods for the determination of polyanhydride phase behavior.
These results were compared with a theoretical phase diagram obtained from Flory-Huggins theory and with atomic force microscopy (AFM) experiments on blend libraries and the agreement between the methods was very good. The high throughput method demonstrates that the CPH/SA system exhibits upper cri...
Synthesis of functionalized isoquinolines via sequential cyclization/cross-coupling reactions.
CuX(2)-mediated cyclization of 2-alkynylbenzaldehyde O-methyl oximes in N,N-dimethylacetamide (DMA) gave rise to 4-chloroisoquinolines in good yield, which underwent the palladium-catalyzed cross-coupling reactions of arylboronic acids subsequently to afford the functionalized isoquinolines.
Rapid combinatorial access to a library of 1,5-disubstituted-3-indole-N-alkylacetamides as CB2 receptor ligands.