172695-25-9Relevant articles and documents
Development of Chiral Organosuperbase Catalysts Consisting of Two Different Organobase Functionalities
Kondoh, Azusa,Oishi, Masafumi,Terada, Masahiro,Tezuka, Hikaru
supporting information, p. 7472 - 7477 (2020/03/19)
In the field of chiral Br?nsted base catalysis, a new generation of chiral catalysts has been highly anticipated to overcome the intrinsic limitation of pronucleophiles that are applicable to the enantioselective reactions. Herein, we reveal conceptually new chiral Br?nsted base catalysts consisting of two different organobase functionalities, one of which functions as an organosuperbase and the other as the substrate recognition site. Their prominent activity, which stems from the distinctive cooperative function by the two organobases in a single catalyst molecule, was demonstrated in the unprecedented enantioselective direct Mannich-type reaction of α-phenylthioacetate as a less acidic pronucleophile. The present achievement would provide a new guiding principle for the design and development of chiral Br?nsted base catalysts and significantly broaden the utility of Br?nsted base catalysis in asymmetric organic synthesis.
A Modular Synthesis of Conformationally Preorganised Extended β-Strand Peptidomimetics
Yamashita, Tohru,Knipe, Peter C.,Busschaert, Nathalie,Thompson, Sam,Hamilton, Andrew D.
supporting information, p. 14699 - 14702 (2015/10/20)
A promising strategy for mediating protein-protein interactions is the use of non-peptidic mimics of secondary structural protein elements, such as the α-helix. Recent work has expanded the scope of this approach by providing proof-of-principle scaffolds that are conformationally biased to mimic the projection of side-chains from one face of another common secondary structural element - the β-strand. Herein, we present a synthetic route that has key advantages over previous work: monomers bearing an amino acid side-chain were pre-formed before rapid assembly to peptidomimetics through a modular, iterative strategy. The resultant oligomers of alternating pyridyl and six-membered cyclic ureas accurately reproduce a recognition domain of several amino acid residues of a β-strand, demonstrated herein by mimicry of the i, i+2, i+4 and i+6 residues.
4-ARYL-BUTANE-1,3-DIAMIDES
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, (2011/07/07)
The invention relates to compound of the formula (I): in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.