- 2-PHENYLNICOTINIC ACID DERIVATIVE
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The present invention is to provide the compounds useful as a treating or preventing agent for gout and hyperuricemia which are 2-phenylnicotinic acid derivatives having a uric acid lowering action due to an excellent xanthine oxidase inhibitory action. Since the 2-phenylnicotinic acid derivatives of the present invention exhibit a uric acid lowering action due to an excellent xanthine oxidase inhibitory action and also hypolipemic action, their utility is very high as a treating or preventive agent for gout and hyperuricemia which are often accompanied by hyperlipemia as a complication.
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- SYNTHESIS OF 3-AMINO-2-CHLORO-4-METHYLPYRIDINE FROM ACETONE AND ETHYL CYANOACETATE
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A method for making 3-amino-2-chloro-4-methylpyridine from acetone and ethyl cyanoacetate, as depicted in the following reaction scheme.
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Page/Page column 5
(2010/02/14)
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- Synthesis of 3-amino-2-chloro-4-methylpyridine from acetone and ethyl cyanoacetate
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A method for making 3-amino-2-chloro-4-methylpyridine from acetone and ethyl cyanoacetate, as depicted in the following reaction scheme.
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- Processes for producing 2-Halo-nicotinic acid derivatives and precursors thereto
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Disclosed are preferred processes for the preparation of 2-halo-nicotinic acid derivatives of formula (IV): STR1 by cyclocondensation of a 4-halo-4-cyanocarbonyl compound of formula (III): STR2 wherein X is Cl or Br; Y is a carbonyl group and R1, R2 and R3 are each, independently, H, Cl, Br or an organic radical. Further preferred aspects include the preparation of the above-noted 4-halo-4-cyanocarbonyl compound via Michael addition of a 2-halonitrile with an α,β-unsaturated aldehyde or ketone, and the preparation of the 2-halonitrile by redistribution of halogen between a 2,2-dihalonitrile and a parent nitrile.
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- Regioselective synthesis of 2-chloro 3-pyridinecarboxylates
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2-Chlorocyanoacetate was found to undergo base-catalyzed Michael addition to α,β-unsaturated ketones or aldehydes to afford 5-oxopentenenitrile derivatives. In the presence of anhydrous HCl, these compounds cyclize to yield 2-chloro-3-pyridinecarboxylates. The process is highly regiospecific and useful in the synthesis of 2,3-disubstituted pyridines.
- Zhang,Stout,Keay,Scriven,Toomey,Goe
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p. 13177 - 13184
(2007/10/03)
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- Preparation of 2-chloropyridine 3-carboxylic acid esters
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2-chloropyridine 3-carboxylic acid esters are prepared by cyclization of 1,3-butadiene derivatives in the presence of hydrogen chloride.
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