- Process for the synthesis of imidazoles
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The present invention provides a process for the preparation of imidazoles by reacting a cyano compound with a silylalkylisocyanide compound. Such imidazoles are useful pharmacologically-active compounds and/or intermediates for the preparation of pharmacologically-active compounds.
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Page/Page column 6
(2008/06/13)
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- Monocyclic, substituted imidazoles as glycosidase inhibitors
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A range of 4-monosubstituted and 2,4-disubstituted 1H-imidazoles and 1H-imidazole-1-ethanols (R-C(4): CH2CH2Ph, CHOHCH 2Ph, Ph, or Me; R-C(2): CH2OH, CHOHCH2OH, CN, or CH2NHAc) were prepare
- Magdolen, Peter,Vasella, Andrea
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p. 2454 - 2469
(2007/10/03)
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- Novel farnesyl protein transferase inhibitors as antitumor agents
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Disclosed are novel tricyclic compounds represented by the formula (1.0): and a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical compositions comprising compounds of formula 1.0. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
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- Synthesis and histamine H3 receptor activity of 4-(n-alkyl)-1H-imidazoles and 4-(omega-phenylalkyl)-1H-imidazoles.
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The influence of lipophilic moieties attached to a 4-1H-imidazole ring on the histamine H3 receptor activity was systematically investigated. Series of 4-(n-alkyl)-1H-imidazoles and 4-(omega-phenylalkyl)-1H-imidazoles were prepared, with an alkyl chain varying from 2-9 methylene groups and from 1-9 methylene groups, respectively. The compounds were tested for their activity on the H3 receptor under in vitro conditions. For the 4-(n-alkyl)-1H-imidazoles the activity is proportional to chain length, ranging from a pA2 value of 6.3 +/- 0.2 for 4-(n-propyl)-1H-imidazole to a pA2 value of 7.2 +/- 0.1 for 4-(n-decyl)-1H-imidazole. For the series 4-(omega-phenylalkyl)-4H-imidazoles an optimum in H3 activity was found for the pentylene spacer: 4-(omega-phenylpentyl)-1H-imidazole has a pA2 value of 7.8 +/- 0.1.
- De Esch,Gaffar,Menge,Timmerman
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p. 3003 - 3009
(2007/10/03)
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- A Two-Step Synthesis of Imidazoles from Aldehydes via 4-Tosyloxazolines
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Imidazoles with substituents in the 4- and 4,5-positions were prepared by heating 4-tosyloxazolines in saturated methanolic ammonia.Similar treatment of these oxazolines with monoalkylamines regioselectively affords 1,4-disubstituted imidazoles.When oxazolines bearing an ethyl group at the 4-position were heated with alkylamines, however, a regioisomeric mixture of di- or trisubstituted imidazoles was produced.These reactions proceed via an intermolecular condensation of α-amino ketones and amidines or intramolecular cyclization of α-amidino ketone intermediates, respectively.
- Horne, David A.,Yakushijin, Kenichi,Buechi, George
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p. 139 - 154
(2007/10/02)
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