- New and general nitrogen heterocycle synthesis: Use of heteropoly acids as a heterogeneous recyclable catalyst
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An efficient synthetic method of six-and five-member nitrogen heterocyclic compounds was developed. Nitrogen heterocyclic compounds were prepared by condensation of the-dicarbonyl compounds with the corresponding-or-amino alcohols, subsequent cyclization, and spontaneous aromatization in the presence of a catalytic amount of Keggin-type heteropoly acids under very mild conditions. Copyright
- Hekmatshoar, Rahim,Sadjadi, Sodeh,Sadjadi, Samaheh,Heravi, Majid M.,Beheshtiha, Yahya S.,Bamoharram, Fatemeh F.
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- Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents
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A novel class of heat shock protein 90 (Hsp90) inhibitors was developed from an unbiased screen to identify protein targets for a diverse compound library. These indol-4-one and indazol-4-one derived 2-aminobenzamides showed strong binding affinity to Hsp
- Huang, Kenneth H.,Veal, James M.,Fadden, R. Patrick,Rice, John W.,Eaves, Jeron,Strachan, Jon-Paul,Barabasz, Amy F.,Foley, Briana E.,Barta, Thomas E.,Ma, Wei,Silinski, Melanie A.,Hu, Mei,Partridge, Jeffrey M.,Scott, Anisa,DuBois, Laura G.,Freed, Tiffany,Steed, Paul M.,Ommen, Andy J.,Smith, Emilie D.,Hughes, Philip F.,Woodward, Angela R.,Hanson, Gunnar J.,McCall, W. Stephen,Markworth, Christopher J.,Hinkley, Lindsay,Jenks, Matthew,Geng, Lifeng,Lewis, Meredith,Otto, James,Pronk, Bert,Verleysen, Katleen,Hall, Steven E.
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experimental part
p. 4288 - 4305
(2010/01/16)
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- Synthesis of 3-Acylpyrroles, 3-(Alkoxycarbonyl)pyrroles, 1,5,6,7-Tetrahydro-4H-indol-4-ones and 3-Benzoylpyridines Based on Staudinger-Aza-Wittig Reactions of 1,3-Dicarbonyl Compounds with 2- and 3-Azido-1,1-dialkoxy- alkanes
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The Staudinger-aza-Wittig reaction of 1,3-dicarbonyl compounds with 2-azido-1,1-diethoxyethane and subsequent cy- clization allowed an efficient synthesis of a variety of pyrroles, 1,5,6,7-tetrahydro-4H-indol-4-ones, and of a pyridine. Georg Thieme Verlag
- Bellur, Esen,Yawer, Mirza A.,Hussain, Ibrar,Riahi, Abdolmajid,Fatunsin, Olumide,Fischer, Christine,Langer, Peter
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experimental part
p. 227 - 242
(2009/06/24)
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- Synthesis of functionalized pyrroles and 6,7-dihydro-1H-indol-4(5H)-ones by reaction of 1,3-dicarbonyl compounds with 2-azido-1,1-diethoxyethane
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The condensation of 1,3-dicarbonyl compounds with 2-azido-1,1- diethoxyethane and subsequent cyclization allowed an efficient synthesis of a variety of pyrroles and 6,7-dihydro-1H-indol-4(5H)-ones.
- Bellur, Esen,Langer, Peter
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p. 2151 - 2154
(2007/10/03)
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- TETRAHYDROINDOLONE DERIVATIVES AS GABAAALPHA5 LIGANDS FOR ENHANCING COGNITION
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Compounds according to Formula (I) or a pharmaceutically acceptable salt thereof are GABA-A Alpha 5 ligands useful for enhancing cognition: where A is C 1-6alkyl, C 2-6alkenyl, C 2-6alkynyl, C 3-6cycloalkyl, arylC 1-6alkyl, or aryl wherein the aryl group is optionally substituted by halogen, C 1-6alkyl, CF 3, CN, NO 2 or NH 2, NR 1R 10, S(O) pR 1, heteroarylC 1-6alkyl or heteroaryl where heteroaryl is a 5-or 6-membered heteroaromatic ring as defined for B; and B is phenyl or a 5-membered ring having one or two unsaturations containing 1, 2, 3, or 4 heteroatoms chosen from O, N and S provided that not more than one heteroatom is other than N, a 6-membered heteroaromatic ring containing 1, 2, 3 or 4 nitrogen atoms, each of which rings is optionally substituted by one or more substituents.
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- Studies on Sugar Nitro-olefins. Part 7. Synthesis of 3-(Alditol-1-yl)-1,2,3,5,6,7-hexahydro- and -1,5,6,7-tetrahydro-indol-4-ones. X-Ray Molecular Structure of (3S)-3-(1,2,3,4,5-Penta-O-acetyl-D-galacto-pentitol-1-yl)-1,2,3,5,6,7-hexahydroindol-4-one
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Raney nickel reduction of (3R)-2-hydroxyimino-3-(1,2,3,4,5-penta-O-acetyl-D-galacto- or -D-glucopentitol-1-yl)-3,5,6,7-tetrahydrobenzofuran-4(2H)-ones (5) gives (3S)-3-(1,2,3,4,5-penta-O-acetyl-D-galacto- or -D-gluco-pentitol-1-yl)-1,2,3,5,6,7-hexahydroindol-4-ones (6) in high yields.Deacetylation of compounds (6) with catalytic sodium methoxide in methanol affords the corresponding (pentitol-1-yl)indolones (7).Compounds (6) can be transformed into the 3-(1,2,3,4,5-penta-O-acetyl-D-galacto- or -D-gluco-pentitol-1-yl)-1,5,6,7-tetrahydroindol-4-ones (8) by treatment with 2,3-dichloro-5,6- dicyano-1,4-benzoquinone.The structure of (3S)-3-(1,2,3,4,5-penta-O-acetyl-D-galacto-pentitol-1-yl)-1,2,3,5,6,7-hexahydroindol-4-one (6a) was confirmed by an X-ray structure determination.
- Dianez, Maria J.,Galan, Jose,Gomez-Sanchez, Antonio,Lopez-Castro, Amparo,Rico, Manuel
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p. 581 - 588
(2007/10/02)
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