32776-22-0Relevant articles and documents
Bifunctional phase-transfer catalysts for fixation of CO2 with epoxides under ambient pressure
Li, Yue-Dan,Cui, Dong-Xiao,Zhu, Jun-Chao,Huang, Ping,Tian, Zhuang,Jia, Yan-Yan,Wang, Ping-An
supporting information, p. 5231 - 5237 (2019/10/11)
A series of bifunctional phase-transfer catalysts with a quaternary onium center and a hydrogen-bonding donor group were prepared for the fixation of CO2 with commercially available epoxides under mild conditions by using a CO2 balloon (1 atm). In the presence of 2.5 mol% of achiral bifunctional phase-transfer catalysts, cyclic carbonates were obtained in good to excellent yields (up to 95%). Additionally, optical carbonates and epoxides were obtained through the kinetic resolution of rac-epoxides by 1 mol% of chiral bifunctional phase-transfer catalysts with low enantioselectivities. These catalysts featured a simple synthetic route, good modularity and high efficiency.
Cyclin-dependent kinase inhibitors and application thereof
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Paragraph 0485; 0490; 0491; 0492, (2018/07/30)
The invention relates to compounds used as cyclin-dependent kinase inhibitors and application thereof, belonging to the field of medical chemistry. Specifically, the invention provides the compound asshown in a formula I which is described in the specification, or isomers, pharmaceutically acceptable salts, solvates, crystals or prodrugs thereof, preparation methods thereof, pharmaceutical compositions containing the compounds, and application of the compounds or the compositions to treatment of cancer, tissue hyperplasia diseases or inflammatory diseases. The compounds of the invention havegood inhibitory activity to CDK7 and are highly expected to be developed into a therapeutic agent for cancer, tissue hyperplasia diseases and inflammatory diseases.
FUSED-RING OR TRICYCLIC ARYL PYRIMIDINE COMPOUND USED AS KINASE INHIBITOR
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Paragraph 0122; 0123, (2018/03/25)
Disclosed is a fused-ring or tricyclic aryl pyrimidine compound used as a mutation selectivity EGFR inhibitor. Specifically, disclosed is a compound represented by formula (I) and used as an EGFR inhibitor or a pharmaceutically acceptable salt thereof.
EGFR INHIBITOR, AND PREPARATION AND APPLICATION THEREOF
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Paragraph 0106; 0683; 0684, (2017/09/02)
A 4-substituted-2-(N-(5-substituted allyl amide)phenyl)amino)pyrimidine derivative as represented by formula (I), and a preparation and application thereof as an EGFR inhibitor. The compound has activity of inhibiting the L858R EGFR mutant, the T790M EGFR mutant and the exon 19 deletion activating mutant, may be used to treat diseases mediated alone or in part by EGFR mutant activity, and has a wide application in drugs preventing and treating cancers, particularly non-small cell lung cancer.
Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors
Ye, Bin,Arnaiz, Damian O.,Chou, Yuo-Ling,Griedel, Brian D.,Karanjawala, Rushad,Lee, Wheeseong,Morrissey, Michael M.,Sacchi, Kama L.,Sakata, Steven T.,Shaw, Kenneth J.,Wu, Shung C.,Zhao, Zuchun,Adler, Marc,Cheeseman, Sarah,Dole, William P.,Ewing, Janice,Fitch, Richard,Lentz, Dao,Liang, Amy,Light, David,Morser, John,Post, Joseph,Rumennik, Galina,Subramanyam, Babu,Sullivan, Mark E.,Vergona, Ron,Walters, Janette,Wang, Yi-Xin,White, Kathy A.,Whitlow, Marc,Kochanny, Monica J.
, p. 2967 - 2980 (2008/02/07)
There remains a high unmet medical need for a safe oral therapy for thrombotic disorders. The serine protease factor Xa (fXa), with its central role in the coagulation cascade, is among the more promising targets for anticoagulant therapy and has been the
Benzotriazine inhibitors of kinases
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Page/Page column 64-65, (2008/06/13)
The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases.
Synthesis, characterization, and biological evaluation of a novel class of N-(arylethyl)-N-alkyl-2-(1-pyrrolidinyl)ethylamines: Structural requirements and binding affinity at the σ receptor
De Costa,Radesca,Di Paolo,Bowen
, p. 38 - 47 (2007/10/02)
By synthesizing and testing a part-structure, N-[2-(3,4- dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamine (3), derived from our previously reported high affinity σ receptor ligands (1S,2R)-(-)-N-[2- (3,4-dichlorophenyl)-ethyl]-N-methyl-2-(1-pyrrolidinyl)cyclohexylamine [(-)- 2] and (+)-2, we have identified a novel class of superpotent (subnanomolar affinity) σ ligands specific for the σ receptor labeled by [3H]-(+)-3-PPP. When 3 was tested for its capacity to displace [3H]-(+)-3-PPP from guinea pig brain membranes, it exhibited a K(i) of 0.34 nM, which is better than either of its parent compounds (-)-2 (K(i) = 1.3 nM) and (+)-2 (K(i) = 6.0 nM). Other compounds related to 3 such as N-[2-(3,4-dichlorophenyl)ethyl]-N- methyl-2-(1-homopiperidinyl)ethylamine (19) exhibited K(i) = 0.17 nM ([3H]- (+)-3-PPP). The determinants for high σ receptor affinity of 3 were examined by manipulation of this structure in a number of different ways. The high efficacy of these compounds for the σ receptor, their relative chemical simplicity and ease of synthesis, and their high degree of selectivity identifies N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1- pyrrolidinyl)ethylamine (3) and related compounds as a highly promising base for determination of the functional role of σ receptors as well as the development of novel therapeutic agents.
Asymmetric synthesis catalyzed by chiral ferrocenylphosphine transition metal complexes. 10 gold(I)-catalyzed asymmetric aldol reaction of isocyanoacetate
Hayashi, Tamio,Sawamura, Masaya,Ito, Yoshihiko
, p. 1999 - 2012 (2007/10/02)
Optically active ferrocenylbisphosphine ligands containing 2-(dialkylamino)ethylamino group on the ferrocenylmethyl position have been prepared and used for the gold(I)-catalyzed asymmetric aldol reaction of isocyanoacetate with aldehydes. Six-membered ring amines, such as morpholino or piperidino group, at the terminal of the side chain were most stereoselective to give optically active trans-4- methoxycarbonyl-5-alkyl-2-oxazolines (up to 97% ee) with high enantio- and diastereoselectivity in a quantitative yield.
2-(3,4-Dichlorophenyl)-N-methyl-N-acetamides: The Use of Conformational Analysis in the Development of a Novel Series of Potent Opioid κ Agonists
Costello, Gerard F.,James, Roger,Shaw, John S.,Slater, Anthony M.,Stutchbury, Neil C. J.
, p. 181 - 189 (2007/10/02)
This paper describes the synthesis of a series of N-acetamides (1), methylated at C1 and/or C2 of the ethyl linking group, and their biological evaluation as opioid κ agonists.Conformational analysis of corresponding desaryl analogues 2 suggested that only those compounds capable of occupying an energy minimum close to that of the known κ agonist N-acetamide U-50488 might possess κ agonist properties.Starting from chiral amino acids, other alkyl and aryl substituents were introduced at C1 of the ethyl-linking moiety, giving compounds capable of adopting the same conformation as U-50488.The most potent of these, 2-(3,4-dichlorophenyl)-N-methyl-N-acetamide (8), was 146-fold more active than U-50488 in vitro in the mouse vas deferens model and exhibited potent naloxone-reversible analgesic effects (ED50 = 0.004 mg/kg sc) in an abdominal constriction model.