- SNAr reaction in aqueous medium in the presence of mixed organic and inorganic bases
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N-Arylation of amines with fluorobenzonitriles in aqueous medium is described. A mixture of N,N-diisopropylethyl amine and Na2CO3 (1:1) is found to achieve maximum conversion by refluxing for 3 hours in water. The product can be easily isolated by solvent extraction.
- Shelke, Nilesh B.,Ghorpade, Ramrao,Pratap, Ajay,Tak, Vijay,Acharya
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p. 31226 - 31230
(2015/04/22)
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- Discovery of novel aminoquinazolin-7-yl 6,7-dihydro-indol-4-ones as potent, selective inhibitors of heat shock protein 90
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A novel class of Hsp90 inhibitors, structurally distinct from previously reported scaffolds, was developed from rational design and optimization of a compound library screen hit. These aminoquinazoline derivatives, represented by compound 15 (SNX-6833) or 1-(2-amino-4-methylquinazolin-7-yl)-3,6,6-trimethyl-6, 7-dihydro-1H-indol-4(5H)-one, selectively bind to Hsp90 and inhibit its cellular activities at concentrations as low as single digit nanomolar.
- Huang, Kenneth H.,Barta, Thomas E.,Rice, John W.,Smith, Emilie D.,Ommen, Andy J.,Ma, Wei,Veal, James M.,Fadden, R. Patrick,Barabasz, Amy F.,Foley, Briana E.,Hughes, Philip F.,Hanson, Gunnar J.,Markworth, Christopher J.,Silinski, Melanie,Partridge, Jeffrey M.,Steed, Paul M.,Hall, Steven E.
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scheme or table
p. 2550 - 2554
(2012/05/20)
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- Isoquinoline, Quinazoline and Phthalazine Derivatives
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Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R0, R5, R6, R7, n, Q1-Q5, Y, and X1-X3 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
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Page/Page column 46
(2008/06/13)
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- Direct Synthesis of 2,4-Diaminoquinazolines from 2-Fluorobenzonitriles
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In a search for new methods for preparing 2,4-diaminoquinazolines having a diversity of substituents in the benzenoid ring, it was found that the reaction of 2,6-difluorbenzonitrile with guanidine carbonate gave 2,4-diamino-5-fluoroquinazoline in excellent yield.Extension of this approach to other 2-fluorobenzonitriles, some of which were elaborated for the first time, showed that this reaction possesses considerable generality.The cyclization was sucessful even when electron donating groups were present at position six.Only in two cases where a primary or secondary amino group was also present ortho to the cyano group was this transformation unsucessful.
- Hynes, John B.,Pathak, Alpana,Panos, Constantina H.,Okeke, Claudia C.
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p. 1173 - 1177
(2007/10/02)
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