- IMIDAZOLE COMPOUNDS AND MEDICINAL USE THEREOF
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Imidazole compounds represented by general formula (I): wherein each symbol is as defined in the specification, and salts thereof, and a pharmaceutical composition containing same are provided. These compounds are useful in treating the diseases curable based on a hypoglycemic action, and the diseases curable based on a cGMP-PDE inhibitory action, a smooth muscle relaxing action, a bronchodilating action, a vasodilating action, a smooth muscle cell inhibitory action and an allergy inhibitory action.
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- New synthetic routes to pyrrolo-[1,2-a]- and -[1,2-c]-imidazol-5-ones by flash vacuum pyrolysis
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1-Substituted and 1,3-disubstituted pyrrolo[1,2-c]imidazol-5-ones 25-27 have been made in fair to excellent yield by flash vacuum pyrolysis (FVP) of the Meldrum's acid precursors 11-13. FVP of the appropriate propenoate precursor 23, 22 and 18-20 gives pyrrolo[1,2-c]imidazol-5-one 2, pyrrolo[1,2-a]-imidazol-5-one 3 and their 6-methyl derivatives 28-30 respectively in 32-90% yield. The mechanism of the propenoate pyrolyses involves rate determining E to Z isomerisation of the alkene followed by elimination of an alcohol and electrocyclisation to the fused ring products.
- McNab, Hamish,Thornley, Craig
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p. 2203 - 2209
(2007/10/03)
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- Synthesis of 4(5)-Acyl-, 1-Substituted 5-Acyl, and 1-Substituted 4-Acyl-1H-imidazoles from 4-Aminoisoxazoles
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4-Aminoisoxazoles can be acylated with a wide variety of activated carboxylic acids.Hydrogenation of the resulting amides gives α-(acylamino)enaminones, which cyclize to 4(5)-acylimidazoles upon treatment with base.This method allows for the synthesis of acylimidazoles with a wide range of substituents at C-2.Utilization of N-substituted 4-aminoisoxazoles in the same sequence of reactions yields 1-substituted 5-acylimidazoles, a substitution pattern not otherwise easily prepared.Treatment of α-(acylamino)enaminones, derived from N-unsubstituted isoxazoles, with primary amines leads to incorporation of the amine at the β-position with concomitant expulsion of ammonia.This sequence efficiently yields 1-substituted and 1,2-disubstituted 4-acylimidazoles but does not give satisfactory yields of 5-substituted 4-acylimidazoles due to steric inhibition of the amine exchange.
- Reiter, Lawrence A.
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p. 2714 - 2726
(2007/10/02)
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- Imidazo[1,5-d]-as-triazine-4(3H)-ones and thiones
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There is provided substituted imidazo[1,5-d]-as-triazine-4(3H)-ones and substituted imidazo[1,5-d]-as-triazin-4(3H)-thiones useful as inhibitors of the enzyme cyclic-AMP phosphodiesterase and as broad spectrum herbicides.
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- Method for the control of undesired plant species using imidazo-as-triazinones and triazine-thiones
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This disclosure describes herbicidal methods for the pre- and postemergence control of undesired mono- and dicotyledonous plants using substituted imidazo[1,5-d]-as-triazin-4(3H)-ones and substituted imidazo[1,5-d]-as-triazine-4(3H)-thiones.
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- SUBSTITUTED 3-(4-IMIDAZOLYLMETHYLENE)CARBAZIC AND THIOCARBAZIC ACID ESTERS
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There are provided substituted 3-(4-imidazolyl-methylene)carbazic acid esters and 3-(4-imidazolylmethylene)dithiocarbazic acid esters useful as intermediates for the preparation of compounds which inhibit the enzyme cyclic-AMP phosphodiesterase
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- IMIDAZO [1,5-d]-AS-TRIAZINE-4(3H)-ONES AND THIONES
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There is provided substituted imidazo[1,5-d]-as-triazine-4(3H)-ones and substituted imidazo[1,5-d]-as-triazin-4(3H)-thiones useful as inhibitors of the enzyme cyclic-AMP phosphodiesterase and as broad spectrum herbicides
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- Imidazo[1,5-d]-as-triazines
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There are provided novel substituted imidazo-[1,5-d]-as-triazines useful as hypotensive agents as well as exhibiting herbicidal activity.
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