Aldehydes react in a disproportionation reaction in the presence of rhodium catalysts to yield amines and amides. By adding N-methylmorpholine N-oxide as an oxidant in the presence of catalytic amounts of rhodium, the oxidative am- [a] 523 ination of aldehydes proceeds selectively to give the corresponding amide. Both aliphatic and aromatic aldehydes react with secondary amines to yield carboxylic acid amides in good to excellent yields.
We synthesized and evaluated by surface plasmon resonance 64 LNA/2 0 -O-methyl sequences corresponding to all possible combinations of such residues in a kissing aptamer loop complementary to the 6-nt loop of the TAR element of HIV-1. Three combinations of LNA/2 0 -O-methyl nucleoside analogues where one or two LNA units are located on the 3 0 side of the aptamer loop display an affinity for TAR below 1 nM, i.e. one order of magnitude higher than the parent RNA aptamer. One of these combinations inhibits the TAR-dependent luciferase expression in a cell assay.
The 2(3)‐formyl‐glycals 2, 4, 6 react with hydrazine hydrate to furnish the C‐(1H‐pyrazol‐3‐yl)alditoles 7, 8, 9. Treatment of 2, 4, 6 with cyanoacetamide provides the 2(3)‐(2‐aminocarbonyl‐2‐cyano‐vinyl)‐1,5(2,6)‐anhydro‐2(3)‐deoxy‐hex‐enitols 10, 13, 15, which are converted into the polyhydroxyalkyl 2‐amino‐nicotinamides 11, 14, 16 and pyridinecarbonitriles 12, respectively.
A novel, long-wavelength, non-fluorescent quencher (LQ), based on 1,4-diaminoanthraquinone, has been incorporated at the 3' and 5'-termini of oligonucleotides. The quencher has been used in Molecular beacons, efficiently quenching the long wavelength fluorophore, Cy5.
Aldehydes react in a disproportionation reaction in the presence of rhodium catalysts to yield amines and amides. By adding N‐methylmorpholine N‐oxide as an oxidant in the presence of catalytic amounts of rhodium, the oxidative amination of aldehydes proceeds selectively to give the corresponding amide. Both aliphatic and aromatic aldehydes react with secondary amines to yield carboxylic acid amides in good to excellent yields.
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