- Regioselective Functionalization of 4-Methyl-1H-indole for Scalable Synthesis of 2-Cyano-5-formyl-4-methyl-1H-indole
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We report a five-step synthesis of 2-cyano-5-formyl-4-methyl-1H-indole through sequential functionalization of readily available 4-methyl-1H-indole. Cyano and aldehyde functionalities are regioselectively installed at the 2 and 5 position, respectively. T
- Zhang, Jun,Hu, Yun,Wang, Haiyu,Guo, Aixin,Kong, Jianshe,Ma, Rujian,Wu, Tao,Wang, Yi,Li, Lian-Sheng,Mai, Wanping,Ren, Pingda,Deng, Xiaohu
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- Three consecutive steps over the chirally modified Pt surface: Asymmetric catalytic cascade reaction of 2-nitrophenylpyruvates
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The influence of the reaction conditions on the asymmetric heterogeneous cascade reaction of 2-nitrophenylpyruvates over Pt catalysts modified with cinchonidine leading to (R)-3-hydroxy-3,4-dihydroquinolin-2(1H)-one derivatives has been studied. Results of studies on the amount of acetic acid or catalyst, nature of the Pt support, kinetic examinations, effect of H2 pressure, and modifier and substrate concentrations showed that all three steps of this catalytic cascade take place on the Pt surface, with the nitro group reduction immediately following the enantioselective hydrogenation of the keto group, whereas the final intramolecular amidation was preceded by desorption after complete reduction of the substrate and re-adsorption of the corresponding intermediate.
- Szollosi, Gy?rgy,Kovcs, Lenke,Makra, Zsolt
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p. 697 - 704
(2015/02/19)
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- ZrCl4-promoted facile synthesis of indole derivatives
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Zirconium(iv) chloride effectively activates nitrogen (N2) extrusion from aryl azidoacrylates followed by annulation to provide the desired indole products in moderate to good yields. The reaction proceeds at low temperature and in short reaction time and is applicable to a variety of substrates.
- Tummatorn,Gleeson,Krajangsri,Thongsornkleeb,Ruchirawat
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p. 20048 - 20052
(2014/05/20)
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- INHIBITORS OF DIACYLGLYCEROL ACYLTRANSFERASE
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful
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Page/Page column 10
(2010/06/19)
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- Heterocyclyl-substituted dihydroquinazolines and their use as antiviral agents
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The invention relates to heterocyclyl-substituted dihydroquinazolines of formula (I), to processes for their preparation, to medicaments containing them, and to methods for the treatment and/or prophylaxis of diseases, in particular, for use as anti-viral agents, in particular, against cytomegaloviruses.
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- Novel triazole derivatives, process for their preparation and pharmaceutical compositions containing them
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The invention relates to a compound of formula in which R1, X1, X2, X3, X4, R4, Y1, Y2 and Y3 are as defined in claim 1. These compounds are CCK-receptor agonists.
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- HETEROCYCLYL-SUBSTITUTED DIHYDROQUINAZOLINES AND USE THEREOF AS AN ANTIVIRAL AGENT
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The invention relates to heterocyclyl-substituted dihydroquinazolines of formula (I), methods for the production and use thereof for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular, for use as anti-viral agents, in particular, against cytomegaloviruses.
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Page/Page column 34-35
(2010/02/09)
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- Tripeptidyl peptidase inhibitors
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The invention is relative to a compound of formula (I) and its use as an inhibitor of the CCK-inactivating peptidase tripeptidyl peptidase (TPP II). The invention concerns in particular the treatment of eating disorder, obesity, psychotic syndrome and associated psychiatric disorders. It concerns also the cosmetic use of a compound (I) in particular to aid slimming.
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Page column 36
(2010/11/29)
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- INDOLE- AND BEZIMIDAZOLE-SUBSTITUTED QUINOLINE DERIVATIVES
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Compounds of the formula STR1 wherein X, R 1, R 2, R 3, R 4, R 5, R 6 and R 7 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
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- Fischer indolization of variously ortho-substituted phenylhydrazones (Fischer indolization and its related compounds. XXV)
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Various kinds of ethyl pyruvate 2-(2-substituted phenyl)hydrazones (1) were subjected to Fischer indolization with acid catalysts. All the phenylhydrazones gave corresponding normal 7-substituted indoles (2). In addition, phenylhydrazones whose ortho-substituent is electron-donative or has a central atom with an unshared electron pair tended to give the 4- or 5- substituted indole (3), which was produced by migration of the ortho- substituent during cyclization, whereas those whose ortho-substituent is electron-attractive tended to give little or no such abnormal product. The kind of acid catalyst used had some effect on the yield ratio of products but not on the kind of products.
- Murakami,Watanabe,Yokoyama,Naomachi,Iwase,Watanabe,Morihata,Okuyama,Kamakura,Takahashi,Atoda,Tojo,Morita,Ishii
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p. 1910 - 1919
(2007/10/02)
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- Formation of Indoles, Isoquinolines, and Other Fused Pyridines from Azidoacrylates
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Mild thermal decomposition in boiling toluene or xylene of the azidocinnamates (1) - (6), readily prepared from the corresponding aldehyde and ethyl azidoacetate, gives indoles in good yield when there is an unsubstituted ortho position, and dihydroisoquinolines, and hence isoquinolines, when there is an o-methyl or methylene group.In the presence of iodine, which seems to favour a radical type process, the yield of isoquinoline is increased, and isoquinoline formation can compete with the indole-forming cyclisation to a free ortho-position.Iodine also catalyses primary enamine formation by a hydrogen abstraction process.The thiophene (7) and pyrazole (8) are formed and decomposed similarly to give the corresponding c-fused pyridines (28) and (29).The 2,6-dichloro compound (9) thermolyses to the stable 2H-azirine (32) which isomerises to the nitrile (33) on stronger heating.Yields in these azide decompositions are sometimes high, though they can be variable and the reactions, though easily carried out, can be complex
- Henn, Lothar,Hickey, Deirde M. B.,Moody, Christopher J.,Rees, Charles W.
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p. 2189 - 2197
(2007/10/02)
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- Synthesis of Isoquinolines from Azidocinnamates; the Effect of Iodine
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Iodine has a marked catalytic effect on the thermolysis of azidocinnamates; indoles, isoquinolines, 1,2-dihydroisoquinolines, or enamines are isolated depending on the conditions.
- Hickey, Deirdre M. B.,Moody, Christopher J.,Rees, Charles W.
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