163061-19-6Relevant articles and documents
ERK INHIBITORS
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Page/Page column 76, (2016/07/05)
The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a method of inhibiting ERK2 in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of Formula (I). The invention also provides a method for treating cancer in a patient in need of such treatment, said method comprising administering to said patient an effective amount of at least one compound of Formula (I).
A rapid and efficient one-pot method for the reduction of N-protected α-amino acids to chiral α-amino aldehydes using CDI/DIBAL-H
Ivkovic, Jakov,Lembacher-Fadum, Christian,Breinbauer, Rolf
supporting information, p. 10456 - 10460 (2015/11/10)
N-Protected amino acids can be easily converted into chiral α-amino aldehydes in a one-pot reaction by activation with CDI followed by reduction with DIBAL-H. This method delivers Boc-, Cbz- and Fmoc-protected amino aldehydes from proteinogenic amino acids in very good isolated yields and complete stereointegrity.
Synthesis of tetrasubstituted symmetrical pyrazines from β-keto γ-amino esters: A mild strategy for self-dimerization of peptides
Kumar, Mothukuri Ganesh,Thombare, Varsha J.,Bhaisare, Rupal D.,Adak, Anindita,Gopi, Hosahudya N.
, p. 135 - 141 (2015/02/02)
A facile synthesis of highly symmetrical tetrasubstituted pyrazines through simple aerial oxidation of β-keto γ-amino esters is reported. The scope of the reaction was examined by use of various amino acid side-chain functional groups andpeptides. The mil
New routes towards reutericyclin analogues
Jones, Raymond C. F.,Bullous, James P.,Law, Carole C. M.,Elsegood, Mark R. J.
, p. 1588 - 1590 (2014/02/14)
A range of N-acylpyrrolo[3,4-c]isoxazoles and derived N-acyltetramides has been prepared via a nitrile oxide dipolar cycloaddition approach, as analogues of the acyltetramic acid metabolite reutericyclin, of interest for its antibiotic potential against G
Hypervalent iodine/TEMPO-mediated oxidation in flow systems: A fast and efficient protocol for alcohol oxidation
Ambreen, Nida,Kumar, Ravi,Wirth, Thomas
, p. 1437 - 1442 (2013/08/23)
Hypervalent iodine(III)/TEMPO-mediated oxidation of various aliphatic, aromatic and allylic alcohols to their corresponding carbonyl compounds was successfully achieved by using microreactor technology. This method can be used as an alternative for the oxidation of various alcohols achieving excellent yields and selectivities in significantly shortened reaction times.
Arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 2: Optimization of P1 and N-aryl
Alper, Phillip B.,Liu, Hong,Chatterjee, Arnab K.,Nguyen, Khanhlinh T.,Tully, David C.,Tumanut, Christine,Li, Jun,Harris, Jennifer L.,Tuntland, Tove,Chang, Jonathan,Gordon, Perry,Hollenbeck, Thomas,Karanewsky, Donald S.
, p. 1486 - 1490 (2007/10/03)
A systematic study of anilines led to the discovery of a metabolically robust fluoroindoline replacement for the alkoxy aniline toxicophore in 1. Investigations of the P1 pocket resulted in the discovery of a wide tolerance of functionality leading to the discovery of 11 as a potent and selective inhibitor of cathepsin S.
Enantiospecific formation of 3,6-dihydro-1H-pyridin-2-ones: Low-pressure palladium-catalysed decarboxylative carbonylation of 3-tosyl-5-vinyloxazolidin- 2-ones
Knight, Julian G.,Lawson, Iain M.,Johnson, Christopher N.
, p. 227 - 230 (2007/10/03)
Palladium-catalysed decarboxylative carbonylation of 3-tosyl-5- vinyloxazolidin-2-ones 5 occurs at atmospheric pressure to give 1-tosyl-3,6-dihydro-1H-pyridin-2-ones 6. The reaction proceeds with no loss of enantiopurity and detosylation with sodium napht
PROCESS FOR PREPARING OXAZOLIDINE DERIVATIVES
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Page/Page column 10-11, (2008/06/13)
A process for preparing (4S,5R)-5-carboxymethyl-2,2-dimethyl-4-phenyl-oxazolidine-3-carboxylic acid t-butyl ester, an intermediate in the preparation of anticancer compounds having a taxane skeleton, such as paclitaxel, docetaxol, etc.
Allylation of aldehydes and imines: Promoted by reuseable polymer-supported sulfonamide of N-glycine
Li, Gui-Long,Zhao, Gang
, p. 633 - 636 (2007/10/03)
A allylation of aldehydes and imines (generated in situ from aldehydes and amines) with allyltributyltin promoted by recoverable and reusable the polymer-supported sulfonamide of N-glycine has been developed. Good to high yields were obtained in various cases. Most of the SnBu3 residue can be recovered as Bu3SnCl. Highly stereoselective synthesis of N-Boc-(2S,3S)-3-hydroxy-2-phenylpiperidine 7 was achieved by using the P4a-mediated allylation of Boc-L-phenylglycinal as a key step.
A direct and efficient stereoconservative procedure for the selective oxidation of N-protected β-amino alcohols
Ocejo, Marta,Vicario, Jose L.,Badía, Dolores,Carrillo, Luisa,Reyes, Efraim
, p. 2110 - 2112 (2007/10/03)
An efficient, very simple and eco-friendly procedure has been developed for the synthesis of highly enantioenriched α-amino aldehydes by IBX-mediated oxidation of the corresponding β-amino alcohols. The procedure has been applied to a wide range of substr