Relevant articles and documents
All total 5 Articles be found
All total 5 Articles be foundThe basicity gradient-driven migration of iodine: Conferring regioflexibility on the substitution of fluoroarenes
Rausis, Thierry,Schlosser, Manfred
, p. 3351 - 3358 (2007/10/03)
Six different fluoroarenes were submitted to the same transformations. Direct deprotonation with alkyllithium or lithium dialkylamide as reagents and subsequent carboxylation afforded the acids 1, 6, 11, 16, 18, and 23. If the aryllithium intermediate was trapped with iodine rather than with dry ice, an iodofluoroarene (2, 7, 12, 17, 19, and 24) was formed. This, upon treatment with lithium diisopropylamide, underwent deprotonation and iodine migration. The resulting new aryllithium species was intercepted either by carboxylation, to give the acids 3, 8, 13, 20, and 25, or by neutralization, to produce the iodofluoroarenes 4, 9, 14, 21, and 26. The latter family of compounds was converted into another set of acids 5, 10, 15, 22, and 27 by subsequent treatment with butyllithium or isopropylmagnesium chloride and carbon dioxide. ( Wiley-VCH Verlag GmbH, 69451 Weinheim, Germany, 2002).
Structure-based drug design of a highly potent CDK1,2,4,6 inhibitor with novel macrocyclic quinoxalin-2-one structure
Kawanishi, Nobuhiko,Sugimoto, Tetsuya,Shibata, Jun,Nakamura, Kaori,Masutani, Kouta,Ikuta, Mari,Hirai, Hiroshi
, p. 5122 - 5126 (2007/10/03)
The design of a novel series of cyclin-dependent kinase (CDK) inhibitors containing a macrocyclic quinoxaline-2-one is reported. Structure-based drug design and optimization from the starting point of diarylurea 2, which we previously reported as a modera
New substituted indolin-2-one derivatives and their use as p39 mitogen-activated kinase inhibitors
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Page/Page column 32, (2009/12/04)
This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.
Indolin-2-one p38α inhibitors III: Bioisosteric amide replacement
Eastwood, Paul,González, Jacob,Gómez, Elena,Caturla, Francisco,Aguilar, Nuria,Mir, Marta,Aiguadé, Josep,Matassa, Victor,Balagué, Cristina,Orellana, Adelina,Domínguez, María
scheme or table, p. 6253 - 6257 (2011/11/29)
Crystallographic structural information was used in the design and synthesis of a number of bioisosteric derivatives to replace the amide moiety in a lead series of p38a inhibitors which showed general hydrolytic instability in human liver preparations. Triazole derivative 13 was found to have moderate bioavailability in the rat and demonstrated potent in-vivo activity in an acute model of inflammation.
Discovery of selective metal-binding peptoids using 19F encoded combinatorial libraries
Pirrung, Michael C.,Park, Kaapjoo
, p. 2115 - 2118 (2007/10/03)
A method for encoding solid-phase split/mix combinatorial libraries using the chemical shift of synthetic fluoroarenes ('F-codes') has been developed. They have wide chemical shift dispersion and are detectable at the sub-μmol level. 19F NMR is
