Document Type and Number:
Japanese Patent JPH0414086
Kind Code:
B2
Abstract:
A process for resolving a racemic modification of beta -adrenergic aryl- or hetaryl-oxypropanolamines such as (+/-)-2-[2-hydroxy-3-[[2-(1_H-indol-3-yl)-1,1-dimethylethyl]amino]prop oxy]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.
Inventors:
RONARUDO DEI DENISU
TERENSU EMU DORAKU
UIRIAMU II KUREIGUBAAMU
TERENSU EMU DORAKU
UIRIAMU II KUREIGUBAAMU
Application Number:
JP16766783A
Publication Date:
March 11, 1992
Filing Date:
September 13, 1983
Export Citation:
Assignee:
SQUIBB BRISTOL MYERS CO
International Classes:
C07D285/10; A61K31/135; A61K31/165; A61P9/12; A61P25/02; C07B31/00; C07B53/00; C07B57/00; C07C67/00; C07C213/00; C07C217/30; C07C219/04; C07C239/00; C07C253/00; C07C255/54; C07C273/16; C07C273/18; C07C275/10; C07C275/22; C07C275/24; C07C313/00; C07C319/20; C07C319/28; C07C321/24; C07C323/20; C07D209/04; C07D209/08; C07D209/14; C07D213/84; C07D401/12
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