FUNCTIONALLY-MODIFIED OLIGONUCLEOTIDES AND SUBUNITS THEREOF
申请人:Sarepta Therapeutics, Inc.
公开号:US20140330006A1
公开(公告)日:2014-11-06
Functionally-modified oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3′ and/or 5′-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.
Facile Synthesis and Isolation of Secondary Amines <i>via</i>
a Sequential Titanium(IV)-Catalyzed Hydroamination and Palladium-Catalyzed Hydrogenation
作者:Erica K. J. Lui、Laurel L. Schafer
DOI:10.1002/adsc.201500861
日期:2016.3.3
alkyl‐substituted secondary amines has been developed. Using a bis(amidate)bis(amido)titanium(IV) precatalyst, the hydroamination of terminal alkynes with a range of amines results in the selective formation of the anti‐Markovnikov product. The crude enamine/imine mixtures are effectively hydrogenated using palladium on carbon (Pd/C) and H2 to afford the corresponding secondary amine in excellent yields.
direct reductive N‐functionalization of aliphatic nitro compounds is presented. The nitro group is partially reduced to a nitrenoid, with a mild and readily available combination of B2pin2 and zinc organyls. Thereby, the formation of an unstable nitroso intermediate is avoided, which has so far severely limited reductive transformations of aliphatic nitro compounds. The reaction is concluded by an electrophilic
A Smiles-type radical rearrangement induced by visible-light-mediated decarboxylation of ω-aryl-N-(acyloxy)phthalimides was developed, giving rise to pharmacologically important substance classes: phenylethylamine derivatives, dihydroisoquinolinones, and benzoazepinones were synthesized on the basis of readily available benzoic acids or benzaldehydes and β- or γ-amino acids. This methodology facilitates
Ruthenium Halide Complexes as
<i>N</i>
‐Alkylation Catalysts
作者:Andrea Rodríguez‐Bárzano、Joel D. A. Fonseca、A. John Blacker、Patrick C. McGowan
DOI:10.1002/ejic.201400117
日期:2014.4
[RuCl2(p-cymene)]2, in the presence of the diphosphine 1,1′-bis(diphenylphosphino)ferrocene (dppf). The best catalytic activities were obtained with ruthenium iodide compounds. The formation of either [RuX(p-cymene)(dppf)][X] or [(RuX2(p-cymene)) 2(dppf)] (X = halide) under the catalytic conditions employed was investigated.