Process for resolution of optical isomers

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United States of America Patent

PATENT NO 4463176
SERIAL NO

06417794

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Abstract

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A process for resolving a racemic modification of .beta.-adrenergic aryl-or hetaryl-oxypropanolamines such as (.+-.)-2-[2-hydroxy-3-[[2-(1H-indol-3-yl)-1,1-dimethylethyl]amino]propoxy]benzonitrile into its individual enantiomers is described. The process comprises converting the racemic modification into a pair of diastereomeric urea derivatives by reaction with a chiral aralkylisocyanate; separation into the individual diastereomers; and facile regeneration of the starting amine by cleavage of the intermediate urea compound using hydrazine. This final step is improved by the addition of an .alpha.-keto carboxylic acid, such as pyruvic acid, which functions as a scavenger of nucleophilic by-products.

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Patent Owner(s)

Patent OwnerAddress
MEAD JOHNSON & COMPANY345 PARK AVE A DE CORP NEW YORK NY 10154

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Dennis, Ronald D Evansville, IN 4 16
Dolak, Terence M Evansville, IN 14 113
Kreighbaum, William E Evansville, IN 9 144

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