- Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones
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A series of spiro hydantoins derived from 8-azachromanones (2,3-dihydro-4H-pyrano[2,3-b]pyridin-4-ones) has been prepared and tested for aldose reductase inhibitory activity. The standard Bucherer-Bergs conditions had to be drastically modified to increas
- Sarges,Goldstein,Welch,Swindell,Siegel,Beyer
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p. 1859 - 1865
(2007/10/02)
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- Azolidinedione derivatives
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A series of novel spiro-deteroazolones derived from a 2,3-dihydropryrano[2,3-b]pyridine ring system have been prepared, including their pharmaceutically acceptable salts. These compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. Typical member compounds include spiro-imides, spiro-oxazolidinediones, spiro-thiazolidinediones and spiro-imidazolidinediones derived from the aforesaid ring system. (4'S) (2'R)-6'-Chloro-2',3'-dihydro-2'-methyl-spiro-[imidazolidine-4,4'-4'H-pyrano[2,3-b]pyridine]-2,5-dione represents a typical and preferred member compound. Methods for preparing all these compounds from known starting materials are provided.
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- AN IMPROVED METHOD OF CHLORINATING 2-ALKOXYNICOTINIC ACIDS
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A novel chlorination process for preparing 5-chloro-2-alkoxynicotinic acids has been developed using commercial 5.25percent sodium hypochlorite (Clorox) as a chlorinating agent.
- Elliott, Mark L.,Goddard, Carl J.
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p. 1505 - 1508
(2007/10/02)
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- Azolidinedione derivatives
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Spiro-heteroazolones of formula wherein, Z is methylene, oxygen, sulfur or imino; Y is oxygen or sulfur; and -A=B-D=E- represents -N=CH-CH=CH-, -CH=N-CH=CH-, -CH=CH-N=CH or -CH=CH-CH=N-, or an N-oxide derivative thereof. These compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. Typical member compounds include spiro-imides, spiro-oxa-zolidinediones, spiro-thiazolidinediones and spiro-imidazolidinediones derived from the aforesaid ring system. (4'S)(2'R)-6'-Chloro-2',3'-dihydro-2'-methyl--spiro-[imidazolidine-4,4'-4'H-pyrano[2,3-b]pyridine]--2,5-dione represents a typical and preferred member compound. Methods for preparing all these compounds from known starting materials are provided.
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- Chlorination of 2-methoxynicotinic acid
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A novel process for chlorinating 2-methoxynicotinic acid at the 5-position of the molecule is disclosed. The process involves the use of an alkali metal hypochlorite as the chlorinating agent in a homogeneous aqueous solvent system. The compound so produced, 5-chloro-2-methoxynicotinic acid, is known to be useful as an intermediate leading to various oral hypoglycemic agents of the benzenesulfonylurea class.
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