246868-60-0Relevant academic research and scientific papers
Development of Chiral Organosuperbase Catalysts Consisting of Two Different Organobase Functionalities
Kondoh, Azusa,Oishi, Masafumi,Terada, Masahiro,Tezuka, Hikaru
, p. 7472 - 7477 (2020)
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.
Resolution of (4RS,5RS)-4,5-diphenylimidazolidine-2-thione using pentafluorophenyl active esters
Andreou, Anna,Shaye, Najla Al,Brown, Hannah,Eames, Jason
experimental part, p. 6935 - 6938 (2011/03/18)
(4RS,5RS)-4,5-Diphenylimidazolidine-2-thione is resolved efficiently by treatment with NaHMDS and an enantiomerically pure pentafluorophenyl active ester. The levels of diastereocontrol were excellent (up to 90% de).
Heterocyclic compounds as P2X7 ion channel blockers
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Page/Page column 28, (2010/02/10)
The present invention relates to a novel series of 4,5-diphenyl-2-amino-4,5-dihydro-imidazole derivatives of the formula II: 1 wherein R, R1, R2, R3, R4, R5, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are P2X7 ion channel blockers and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases having an inflammatory component, including inflammatory bowel disease, rheumatoid arthritis and disease conditions associated with the central nervous system, such as stroke, Alzheimer''s disease, etc.
The efficient enantiodivergence of (dl)-1,3-diacetyl-2- imidazolidinethiones by enantioselective catalytic deacetylation
Yokoyama, Kazuhiro,Ishizuka, Tadao,Kunieda, Takehisa
, p. 6285 - 6288 (2007/10/03)
An enantioselective borane-mediated deacylation of C2- symmetrical 1,3- diacetyl-2-imidazolidinethiones, catalyzed by oxazaborolidines derived in situ from an aminoalcohol 2 and borane, provides a promising process for highly effective kinetic
