128460-74-2Relevant academic research and scientific papers
A Highly Efficient Monophosphine Ligand for Parts per Million Levels Pd-Catalyzed Suzuki–Miyaura Coupling of (Hetero)Aryl Chlorides
Choy, Pui Ying,Yuen, On Ying,Leung, Man Pan,Chow, Wing Kin,Kwong, Fuk Yee
, p. 2846 - 2853 (2020/04/09)
A new indolylphosphine WK-phos has been synthesized for Pd-catalyzed Suzuki–Miyaura coupling of (hetero)aryl chlorides with (alkyl)arylboronic acids. Comprising this newly developed ligand with palladium(II) acetate, the resulting catalyst system was found to be highly effective in facilitating the reaction even when the catalyst loading reaches parts per million levels (e.g. 10 ppm). These examples represent one of the lowest catalyst loadings reported to date of employing monophosphine (e.g. Ar-PCy2) for Suzuki–Miyaura reactions. The ligand geometry has also been well-characterized by single-crystal X-ray crystallography.
Phosphine ligand for indole skeleton as well as preparation method and application of phosphine ligand
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Paragraph 0221-0226, (2017/12/30)
The invention provides a phosphine ligand for a 3-(disubstituted phosphino)-1-alkyl-2-substituted phenyl-indole skeleton as well as a preparation method and application of the phosphine ligand. The structure of the phosphine ligand for the 3-(disubstituted phosphino)-1-alkyl-2-substituted phenyl-indole skeleton is shown as the following formula I: (shown in the description), wherein Z is carbon or nitrogen, R is alkyl, substituted alkyl, olefin, aryl or fluorine, R1 is alkyl, substituted alkyl or aryl, R2 is alkyl, substituted alkyl or fluorine, and R3 is alkyl, substituted alkyl or aryl.
AROMATIC ESTERS AND POLYESTERS, PRODUCTION WITHOUT ESTERIFICATION CATALYST, AND USE
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Paragraph 0058, (2018/04/12)
This disclosure relates to methods for production of aromatic esters useful as plasticizers without using esterification catalyst, to the aromatic esters, and to polymer compositions containing the aromatic esters. It also relates to producing aromatic polyesters without using esterification catalyst. The aromatic esters and polyesters can be produced catalyst-free by esterifying carboxylic acids with alcohol(s) at high temperature and high pressure, namely at a temperature from 100°C to 350°C and a pressure ≥ 100 psig, preferably ≥ 600 psig. The aromatic esters and polyesters can also be produced by esterifying without esterification catalyst carboxylic acids with methyl or ethyl alcohol, separating the resulting methyl or ethyl esters from the carboxylic acid and any byproduct impurities, and then transesterifying with or without esterification catalyst the methyl or ethyl esters with alcohols and/or diols.
Inhibitors of prenyl transferases
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, (2008/06/13)
Compounds which inhibit prenyl transferases, particularly farnysyltransferase and geranylgeranyl transferase I, processes for preparing the compounds, pharmaceutical compositions containing the compounds, and methods of use.
Design and synthesis of non-peptide Ras CAAX mimetics as potent farnesyltransferase inhibitors
Qian, Yimin,Vogt, Andreas,Sebti, Sa?d M.,Hamilton, Andrew D.
, p. 217 - 223 (2007/10/03)
Cysteine farnesylation of the ras oncogene product Ras is required for its transforming activity and is catalyzed by farnesyltransferase (FTase). The Ras carboxyl terminal tetrapeptide CAAX (C is cysteine, A is any aliphatic amino acid, X is methionine or serine) is the minimum sequence for FTase recognition. We report here the design, synthesis, and biological characterization of Ras CAAX non-peptide mimetics in which the cysteine is linked through a reduced pseudopeptide bond to 4-amino-3'-carboxybiphenyl. These non-peptide mimetics are potent inhibitors of FTase (IC50 = 40 nM for the most potent inhibitor) and are highly selective for FTase over GGTase I (geranylgeranyltransferase I). They are not substrates for farnesylation, do not have peptidic features, and have no hydrolyzable bonds. Structure- activity studies reveal the importance of the position of the carboxylic acid on the aryl ring as well as the reduction of the cysteine amide bond. Substitution at the 2-position of 4-amino-3'-carboxybiphenyl increases inhibitory potency, while the removal of the carboxylic acid results in a 10- fold loss of inhibitory activity.
SYNTHESIS AND BIOLOGICAL ACTIVITIES OF NEW HMG-COA SYNTHASE INHIBITORS: 2-OXETANONES WITH A SIDE CHAIN CONTAINING BIPHENYL, TERPHENYL OR PHENYLPYRIDINE
Hashizume, Hirokazu,Ito, Hajime,Kanaya, Naoaki,Nagashima, Hajime,Usui, Hiroyuki,et al.
, p. 1551 - 1572 (2007/10/02)
A series of 1233A analogs containing biphenylyl, terphenylyl or phenylpyridyl groups in their side chain were synthesized and tested for the inhibitory activities against 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) synthase and inhibition for the chol
