85612-60-8Relevant academic research and scientific papers
Bianthryl-based organocatalysts for the asymmetric Henry reaction of fluoroketones
Otevrel, Jan,Svestka, David,Bobal, Pavel
supporting information, p. 5244 - 5248 (2019/06/07)
We have developed a catalytic system based on bianthrylbis(thiourea) for the asymmetric Henry reaction of fluoroketones and nitroalkanes that resulted from the screening of a library containing 31 chiral non-racemic organocatalysts. The corresponding adducts were isolated in up to 6 times shorter reaction time in comparison with the previously published organocatalysts. High levels of stereocontrol have been generally observed, with measured product enantiomeric excesses up to 97% and diastereomeric ratio 3:2 (anti/syn). The above-mentioned catalysts have been successfully applied to the total asymmetric synthesis of CF3-tethered (S)-halostachines, which has proved that this method constitutes an easy entry to similar enantiopure compounds.
Palladium-Catalyzed Modular Synthesis of Substituted Piperazines and Related Nitrogen Heterocycles
Montgomery, Thomas D.,Rawal, Viresh H.
supporting information, p. 740 - 743 (2016/03/01)
We report here a novel method for the modular synthesis of highly substituted piperazines and related bis-nitrogen heterocycles via a palladium-catalyzed cyclization reaction. The process couples two of the carbons of a propargyl unit with various diamine components to provide nitrogen heterocycles in generally good to excellent yields and high regio- and stereochemical control. (Chemical Equation Presented).
Application of aziridinium ring opening for preparation of optically active diamine and triamine analogues: highly efficient synthesis and evaluation of DTPA-based MRI contrast enhancement agents
Sun, Xiang,Chen, Yunwei,Wu, Ningjie,Kang, Chi Soo,Song, Hyun A.,Jin, Shengnan,Fu, Yao,Bryant, Henry,Frank, Joseph A.,Chong, Hyun-Soon
, p. 94571 - 94581 (2015/11/23)
Ring opening of aziridinium ions with nitrogen nucleophiles was applied to the highly efficient synthesis of optically active vicinal diamines and diethylene triamine pentaacetic acid (DTPA) analogues as potential magnetic resonance imaging (MRI) contrast enhancement agents. The synthetic method features a column-free isolation of the regiospecific and stereospecific nucleophilic substitution products of enantiomerically enriched aziridinium ions in excellent yield.
Phenylalanine-Derived Imidazolines Bearing Heteroaromatic Pendants: Synthesis, Characterization, and Application in the Asymmetric Henry Reaction
Tydlitát, Ji?í,Bure?, Filip,R??i?ková, Zdeňka
, p. 1351 - 1363 (2015/10/28)
Starting from L-phenylalanine, (2S)-3-phenylpropane-1,2-diamine has been prepared and used as building block for the construction of the imidazoline ring. Four new optically pure NH-imidazolines bearing different six-membered heteroaromatic substituents o
CHIRAL FLUORINATING REAGENTS
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Page/Page column 42, (2014/05/24)
This invention relates to fluorinating agents and, more particularly, to chiral non-racemic fluorinating agents useful for enantioselective fluorination, as well as to their synthesis and use and other subject matter. The fluorinating agents are based on a substituted 1,4-diazabicyclo[2.2.2]octane (DABCO) skeleton and provide electrophillic fluorine enantioselectively.
Adenosine-binding motif mimicry and cellular effects of a thieno[2,3-d]pyrimidine-based chemical inhibitor of atypical protein kinase C isoenzymes
Kjaeaer, Svend,Linch, Mark,Purkiss, Andrew,Kostelecky, Brenda,Knowles, Phillip P.,Rosse, Carine,Riou, Philippe,Soudy, Christelle,Kaye, Sarah,Patel, Bhavisha,Soriano, Erika,Murray-Rust, Judith,Barton, Caroline,Dillon, Christian,Roffey, Jon,Parker, Peter J.,Mcdonald, Neil Q.
, p. 329 - 342 (2013/06/05)
The aPKC [atypical PKC (protein kinase C)] isoforms ? and ζ play crucial roles in the formation and maintenance of cell polarity and represent attractive anti-oncogenic drug targets in Ras-dependent tumours. To date, few isoform-specific chemical biology
THIENOPYRIMIDINE INHIBITORS OF ATYPICAL PROTEIN KINASE C
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Page/Page column 198-199, (2013/06/06)
The present invention provides a compound of formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, R6, A, G, M, Q and X are as defined herein. A compound of formula (I) and its salts h
ORGANIC COMPOUNDS
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Page/Page column 68-69, (2010/01/30)
The present invention provides heterocyclicderivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
ORGANIC COMPOUNDS
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Page/Page column 105, (2008/12/08)
The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
Asymmetric catalysis of carbon-carbon bond forming reactions using amino acid-derived C1-symmetrical salen ligands
Belokon, Yuri N.,Hunt, Jamie,North, Michael
experimental part, p. 2804 - 2815 (2009/06/28)
Four amino acids (alanine, valine, phenylalanine and phenylglycine) have been converted into C1-symmetrical salen ligands and complexed to titanium, vanadium, copper and cobalt. The resulting complexes have been used as asymmetric catalysts for asymmetric cyanohydrin synthesis, asymmetric Strecker reactions, asymmetric synthesis of α-methyl amino acids and asymmetric Darzens condensations. Satisfactory levels of asymmetric induction were obtained from reactions in which the (salen)metal complex acts as a chiral Lewis acid, but low levels of asymmetric induction were obtained from reactions carried out under solid-liquid phase-transfer conditions.
