- Radical-promoted site-specific cross dehydrogenative coupling of heterocycles with nitriles
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A first free-radical triggered site-specific cross dehydrogenative coupling reaction of heterocycles with simple nitriles is developed. It allows efficient and facile access to various C-2 cyanoalkylated furans, thiophenes, indoles, and pyrroles. The extremely high selectivities in this case indicate that functionalization of an inert C-H bond could be well-controlled by radical initiation.
- Liu, Zhong-Quan,Li, Zejiang
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- 1,3,6-trihydro-6-aza-3-oxapentalen-2-one derivatives for the treatment of neoplasia
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1,3,6-Trihydro-6-Aza-3-Oxapentalen-2-One Derivatives for inhibiting neoplastic conditions.
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- Simple synthetic approach to arylacetic NSAIAs via TosMIC procedure
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Preparation of 1-methylpyrrole-2-acetonitrile, 1-methyl-5-(4-methylbenzoyl) pyrrole-2-acetonitrile and 2-(6-methoxy-2-naphthyl)propionitrile by treatment of 1-methylpyrrole-2-carboxaldehyde, 1-methyl-5-(4-methylbenzoyl)pyrrole-2-carboxaldehyde and, respectively, 6-methoxy-2-acetylnaphthalene with tosylmethylisocyanide (TosMIC) is described. This one-step synthetic procedure is very useful to obtain the nitrile precursors of tolmetin and naproxen, two clinically important non-steroidal antiinflammatory agents (NSAIAs).
- Di Santo,Costi,Massa,Artico
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p. 787 - 793
(2007/10/02)
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- Preparation of 5-aroyl-1-loweralkylpyrrole-2-acetic acid derivatives
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Known types of 5-aroyl-1-loweralkylpyrrole-2-acetic acid derivatives are prepared by the thermal reaction of an aroylcyanide with a 1-alkylpyrrole-2-acetic acid derivative.
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- Preparation of 5-aroyl-pyrrole compounds
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A process for acylating pyrrole compounds comprising reacting an aroyl halide with the pyrrole compound in the presence of an alkyl aluminum halide. Such acylated pyrrole derivatives are useful as intermediates for the preparation of anti-inflammatory agents and as synthetic intermediates.
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- Preparation of 5-aroylpyrrole-2-acetic acid derivatives
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The interaction of a 2-aryldithiolanium cation with an appropriate pyrrole-2-acetic acid derivative to give a 5-[2-aryl-2-(1,3-dithiolanyl)]pyrrole-2-acetic acid derivative which is then converted to the corresponding 5-aroylpyrrole-2-acetic acid derivative.
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- Uncatalyzed aroylation of 1-alkylpyrrole-2-acetic acid derivatives
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A process of aroylating 1-alkylpyrrole-2-acetic acid esters and nitriles without employing the usual Friedel-Crafts of catalyst.
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- 5-Chlorocarbonyl
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A process of preparing certain 5-aroyl-pyrrole-2-alkanoic acid derivatives using phosgene and certain 5-unsubstituted pyrroles as starting materials, and certain novel 5-chlorocarbonyl-pyrrole precursors.
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- Aroyl-substituted pyrroles
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The compounds are of the class of 5-aroyl-pyrrole alkanoic acids and corresponding acid derivatives thereof useful as anti-inflammatory agents and as synthetic intermediates.
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- Preparation of toluoyl-5-pyrryl-2-acetonitrile
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A process for preparing a mixed anhydride acylating agent and a process for acylating pyrrole derivatives, such as 1-methylpyrrole-2-acetonitrile using the mixed anhydride acylating agent.
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